Anti-ulcer pyridyloxy derivatives, their preparation and uses

ABSTRACT

Compounds of formula (I): ##STR1## [wherein: R 1  is a cyclic amino group, or a dialkylamino group; R 2  a group of formula --NHCHR 3  R 4  wherein R 3  and R 4  are each alkyl aryl or aralkyl, or together form a cycloalkyl group, or R 2  is an aromatic heterocyclic group, or a group of formula --B--S(O) m  --R 5  wherein R 5  is a substituted alkyl group, or an aromatic heterocyclic group; B is an alkylene or alkylidene group; m is 0, 1 or 2; A is a group of formula --CH═CH-- or --(CH 2 ) n  --, where n is 1, 2 or 3]; and salts thereof have valuable anti-ulcer activity.

BACKGROUND TO THE INVENTION

The present invention relates to a series of new pyridyloxy derivativeswhich have the ability to inhibit the secretion of gastric juices andwhich may thus be used for the treatment and prevention of ulcers. Theinvention also provides methods and compositions using these newcompounds for such treatment and prevention and processes for thepreparation of these compounds.

Peptic ulcers are said to occur when there is an imbalance betweenfactors which attack the gastro-intestinal mucosa and factors whichdefend the gastrointestinal mucosa. The gastric juice is among theattacking factors. Accordingly, if its secretion could be inhibited,this would be useful for the prevention and therapy of ulcers.

Among the drugs so far proposed for the inhibition of gastric juicesecretion, anticholinergic agents and histamine-H₂ receptor antagonists(such as cimetidine) have been widely used clinically and have hadconsiderable success, although they are not free from disadvantages. Forexample, anticholinergic agents have exhibited a range of side effects,including inhibition of movement of the gastrointestinal tract, thirst,mydriasis and inhibition of sweating. Some of the histamine-H₂ receptorantagonists also have undesirable side effects on the central nervoussystem, and may also have an antagonistic effect on androgens. Moreover,it is thought that the histamine-H₂ receptor antagonists may weakenmucosal protecting factors after long-term administration, andrecurrence of ulcers after withdrawal of these drugs has also beenobserved. Since recurrence is thought to be caused by a decrease in theprotecting factors, a drug having the ability both to inhibit gastricjuice secretion and to potentiate protecting factor activity would behighly desirable.

We have now discovered that a series of pyridyloxy derivatives having acertain specific and limited class of substituents has the desiredcombination of gastric juice secretion inhibitory activity, anti-ulceractivity and defense factor potentiating activity, and may therefore beused in the treatment and prevention of gastric ulcers.

A number of compounds having anti-ulcer activity and similar structuresto the pyridyloxy derivatives of the present invention is known.Examples include Compound A (disclosed, for example, in European PatentPublication No. 404 949 or WO90/00544), Compound B (disclosed, forexample, in Japanese Patent Kokai Application No. Hei-1-193247, JapanesePatent Kokai Application No. Sho-63-225371 and European PatentPublication No. 282 077) and Compound C (disclosed, for example, inJapanese Patent Kokai Application No. Hei-4-257581): ##STR2##

Compound C was disclosed after the priority dates hereof. The compoundsof the present invention surprisingly have substantially betteractivities than these structurally similar and have a combination ofgastric juice secretion inhibitory, anti-ulcer and defense factorpotentiating activities which these prior compounds do not possess.

BRIEF SUMMARY OF INVENTION

It is, therefore, an object of the present invention to provide a seriesof new pyridyloxy derivatives.

It is a further, and more specific object of the invention to providesuch compounds which may be useful for the treatment and/or preventionof gastric ulcers.

Other objects and advantages of the invention will become apparent asthe description proceeds.

The compounds of the present invention are those compounds of formula(I): ##STR3## wherein: R¹ represents

a cyclic amino group having from 3 to 7 ring atoms, of which from 1 to 3are nitrogen atoms, 0 or 1 is an oxygen atom or a sulfur atom, and theremainder are carbon atoms, or

a dialkylamino group in which each alkyl group is independently selectedfrom the group consisting of alkyl groups having from 1 to 4 carbonatoms;

R² represents

a group of formula --NHCHR³ R⁴, wherein

R³ and R⁴ are independently selected from the group consisting of alkylgroups having from 1 to 6 carbon atoms, aryl groups as defined below andaralkyl groups as defined below, or

R³ and R⁴ together with the carbon atom to which they are attached,represent a cycloalkyl group having from 3 to 8 ring carbon atoms, whichgroup is unsubstituted or is substituted by at least one substituentselected from the group consisting of substituents α,

an aromatic heterocyclic, group having 5 ring atoms, of which from 1 to3 are hetero-atoms selected from the group consisting of nitrogen,oxygen and sulfur hetero-atoms, said group being unsubstituted or havingat least one substituent selected, in the case of substituents on carbonatoms, from the group consisting of substituents α and, in the case ofsubstituents on nitrogen atoms, from the group consisting ofsubstituents β,

or a group of formula --B--S(O)_(m) --R⁵, wherein

R⁵ represents: a substituted alkyl group which has from 1 to 4 carbonatoms and which is substituted by at least one substituent selected fromthe group consisting of substituents γ; or an aromatic heterocyclicgroup which has 5 or 6 ring atoms of which from 1 to 4 are hetero-atomsselected from the group consisting of nitrogen, oxygen and sulfurhetero-atoms, said group being unsubstituted or having at least onesubstituent selected, in the case of substituents on carbon atoms, fromthe group consisting of substituents α and, in the case of substituentson nitrogen atoms, from the group consisting of substituents ε,

B represents an alkylene or alkylidene group having from 1 to 6 carbonatoms,

and m is 0, 1 or 2;

A represents a group of formula --CH═CH-- or --(CH₂)_(n) --, where n is1, 2 or 3;

said aryl groups are carbocyclic aromatic groups having from 6 to 10ring carbon atoms which are unsubstituted or which are substituted by atleast one substituent selected from the group consisting of substituentsζ;

said aralkyl groups are alkyl groups which have from 1 to 4 carbon atomsand which are substituted by from 3 aryl groups as defined above;

said substituents α are selected from the group consisting of: alkylgroups having from 1 to 4 carbon atoms; alkoxy groups having from 1 to 4carbon atoms; hydroxy groups; halogen atoms; amino groups;monoalkylamino groups in which the alkyl part has from 1 to 4 carbonatoms; dialkylamino groups in which each alkyl part is independentlyselected from the group consisting of alkyl groups having from 1 to 4carbon atoms; alkanoylamino groups having from 1 to 5 carbon atoms;arylcarbonylamino groups in which the aryl part is as defined above; andaryl groups as defined above;

said substituents β are selected from the group consisting of alkylgroups having from 1 to 4 carbon atoms;

said substituents y are selected from the group consisting of: hydroxygroups; alkanoyloxy groups having from 1 to 5 carbon atoms; substitutedalkanoyloxy groups which have from 2 to 5 carbon atoms and which aresubstituted by at least one substituent selected from the groupconsisting of substituents δ; arylcarbonyloxy groups in which the arylpart is as defined above; and cycloalkylcarbonyloxy groups in which thecycloalkyl part has from 3 to 6 ring carbon atoms and is unsubstitutedor is substituted by at least one substituent selected from the groupconsisting of substituents α;

said substituents δ are selected from the group consisting of: carboxygroups; alkoxycarbonyl groups in which the alkoxy part has from 1 to 4carbon atoms; aryloxycarbonyl groups in which the aryl part is asdefined above; and aryl groups as defined above;

said substituents ε are selected from the group consisting of: alkylgroups having from 1 to 4 carbon atoms; and hydroxyalkyl groups havingfrom 2 to 4 carbon atoms;

said substituents ζ are selected from the group consisting ofsubstituents α, provided that any aryl group in said substituents α isnot further substituted by an aryl group;

PROVIDED THAT, when m is 1, R⁵ represents: said substituted alkyl grouphaving from 1 to 4 carbon atoms; an aromatic heterocyclic group whichhas 5 ring atoms of which from 2 to 4 are hetero-atoms selected from thegroup consisting of nitrogen, oxygen and sulfur hetero-atoms, said groupbeing unsubstituted as defined above or an aromatic heterocyclic groupwhich has 6 ring atoms of which from 1 to 4 are hetero-atoms selectedfrom the group consisting of nitrogen, oxygen and sulfur hetero-atoms,said group being unsubstituted as defined above;

and pharmaceutically acceptable salts thereof.

The invention also provides a pharmaceutical composition for thetreatment and prophylaxis of ulcerous conditions, which comprises ananti-ulcer compound in admixture with a pharmaceutically acceptablecarrier or diluent, wherein the anti-ulcer compound is selected from thegroup consisting of compounds of formula (I) and pharmaceuticallyacceptable salts thereof.

The invention still further provides a method for the treatment andprophylaxis of ulcerous conditions, which comprises administering aneffective amount of an anti-ulcer compound to a mammal, wherein theanti-ulcer compound is selected from the group consisting of compoundsof formula (I) and pharmaceutically acceptable salts thereof.

The present invention also provides processes for preparing thesecompounds, which are described in greater detail hereafter.

DETAILED DESCRIPTION OF INVENTION

In the compounds of the present invention, where R¹ represents a cyclicamino group, this has from 3 to 7 ring atoms, including at least onenitrogen atom. In addition, there may be another 1 or 2 nitrogen atomsand/or an oxygen or sulfur atom. The group is attached to the methylenegroup forming part of the remainder of the molecule by means of anitrogen atom. The group preferably has a single nitrogen atom, theremainder of the ring atoms being carbon. Examples of such groupsinclude the 1-aziridinyl, 1-azetidinyl, 1-pyrrolidinyl, piperidino and1-hexahydroazepinyl groups. Of these we prefer the 1-pyrrolidinyl andpiperidino groups, more preferably the piperidino group.

Where R¹ represents a dialkylamino group or substituent α, β, ε or ζrepresents an alkyl group, this alkyl group may be a straight orbranched chain alkyl group having from 1 to 4 carbon atoms, and examplesinclude the methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyland t-butyl groups, preferably the methyl, ethyl, propyl, isopropyl,butyl and sec-butyl groups, and most preferably the methyl or ethylgroup.

In the case of the dialkylamino group represented by R¹, the two alkylgroups may be the same or different although they are preferably thesame. Specific examples of dialkylamino groups include thedimethylamino, diethylamino, dipropylamino, diisopropylamino,dibutylamino, dipentylamino, dihexylamino, methylethylamino andmethylpropylamino, of which we prefer the dimethylamino, diethylaminoand dipropylamino groups, especially the dimethylamino group.

Where R² represents a group of formula --NHCHR³ R⁴ and R³ and/or R⁴represents an alkyl group having from 1 to 6 carbon atoms, this may be astraight or branched chain group having from 1 to 6, preferably from 1to 4, carbon atoms, and examples include the methyl, ethyl, propyl,isopropyl, butyl, isobutyl, sec-butyl, t-butyl, pentyl, isopentyl,neopentyl, 2-methylbutyl, 1-ethylpropyl, 4-methylpentyl, 3-methylpentyl,2-methylpentyl, 1-methylpentyl, 3,3-dimethylbutyl, 2,2-dimethylbutyl,1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl,2,3-dimethylbutyl, 2-ethylbutyl, hexyl and isohexyl groups. Of these, weprefer the methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, pentyland hexyl groups, and most prefer the methyl and ethyl groups.

Where R² represents a group of formula --NHCHR³ R⁴ and R³ and/or R⁴represents an aryl group, this has from 6 to 10, preferably 6 or 10,ring carbon atoms and may be unsubstituted or it may be substituted byone or more of substituents ζ, defined above and exemplified below.Specific examples of the unsubstituted aryl groups include the phenyland naphthyl (1- or 2- naphthyl) groups, of which the phenyl group ispreferred. The aryl ring may optionally have one or more substituents(preferably from 1 to 3 substituents, and more preferably 1substituent). Examples of such substituents are given in more detailbelow, but the preferred substituents are alkyl groups having from 1 to4 carbon atoms, alkoxy groups having from 1 to 4 carbon atoms, andhalogen atoms (such as the fluorine, chlorine, bromine or iodine atoms).Preferred substituents are the methyl group, the methoxy group, thefluorine atom and the chlorine atom. The substituents are, in the caseof substituted phenyl groups, preferably on the 4-position. Examples ofpreferred substituted phenyl groups include the 4-methylphenyl,4-methoxyphenyl, 4-chlorophenyl and 4-fluorophenyl groups.

Where R² represents a group of formula --NHCHR³ R⁴, and R³ and/or R⁴represents an aralkyl group, the aryl part may be as exemplified aboveand the alkyl part may be any one of those alkyl groups having from 1 to4 carbon atoms exemplified above. Preferably the aryl and alkyl parts ofthe aralkyl group together have from 7 to 11 carbon atoms. The aryl partof the aralkyl group may be substituted or unsubstituted, and, ifsubstituted, the substituents are selected from the group consisting ofsubstituents ζ defined above and exemplified below. However, the groupis preferably unsubstituted. Examples of such aralkyl groups include thebenzyl, phenethyl, 1-phenylethyl, 2-phenylpropyl, 3-phenylpropyl,4-phenylbutyl and 1- and 2- naphthylmethyl groups, of which the benzyl,phenethyl and 1- and 2- naphthylmethyl groups are preferred, the benzylgroup being most preferred.

Where R² represents a group of formula --NHCHR³ R⁴ and R³ and R⁴together with the carbon atom to which they are attached, represent acycloalkyl group, this has from 3 to 8 ring carbon atoms, and examplesinclude the cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,cycloheptyl and cyclooctyl groups, of which the cyclopropyl, cyclobutyland cyclopentyl groups are preferred, and the cyclopropyl and cyclobutylgroups are most preferred. The cycloalkyl ring may be substituted orunsubstituted, and, if substituted, it preferably has from 1 to 3, morepreferably 1, substituents selected from the group consisting ofsubstituents α. Examples of such substituents are given in more detailbelow, but the preferred substituents are alkyl groups having from 1 to4 carbon atoms and alkoxy groups having from 1 to 4 carbon atoms. Ofthese, we prefer the methyl or ethyl group, but the cycloalkyl group ispreferably unsubstituted.

Where R² represents an aromatic heterocyclic group, this has 5 ringatoms, of which from 1 to 3 are hetero-atoms selected from oxygen,nitrogen and sulfur atoms. Where there is one hetero-atom, this may beany of the oxygen, nitrogen and sulfur atoms. Where there are two orthree hetero-atoms, we prefer that all three or two should be nitrogenatoms and none or one should be an oxygen or sulfur atom. Examples ofsuch groups include the furyl, thienyl, pyrrolyl, oxazolyl, isoxazolyl,thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,2,3-, 1,2,4-, 1,2,5-,or 1,3,4-oxadiazolyl, 1,2,3-, 1,2,4-, 1,2,5- or 1,3,4thiadiazolyl, and1,2,3- or 1,2,4-triazolyl groups. Of these, the furyl, thienyl,pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolyl, imidazolyl and1,2,3-thiadiazolyl groups are preferred, and the thienyl, thiazolyl,pyrrolyl, pyrazolyl and 1,2,3-thiadiazolyl groups are more preferred. Weparticularly prefer the thienyl, pyrrolyl and pyrazolyl groups. Thesegroups may be unsubstituted or they may be substituted by one or moresubstituents. Where the substituent is on a carbon atom, it may beselected from the group consisting of substituents α, defined above andexemplified below. Where the substituent is on a nitrogen atom, it maybe selected from the group consisting of substituents β, defined aboveand exemplified below. There is no particular limitation on the numberof such substituents, except that the number of substitutable positionson 5-membered aromatic heterocyclic groups is 4, and from 1 to 4 suchsubstituents are possible, from 1 to 3 being preferred and 1 or 2 beingmost preferred.

Examples of substituents α include:

alkyl groups having from 1 to 4 carbon atoms, as exemplified above;

alkoxy groups having from 1 to 4 carbon atoms, such as the methoxy,ethoxy, propoxy, isopropoxy, butoxy and isobutoxy groups, of which themethoxy and ethoxy groups are preferred;

hydroxy groups;

halogen atoms, such as the fluorine, chlorine, bromine and iodine atoms,of which the fluorine and chlorine atoms are preferred;

amino groups;

monoalkylamino groups in which the alkyl part has from 1 to 4 carbonatoms, such as the methylamino, ethylamino, propylamino, isopropylamino,butylamino and isobutylamino groups, preferably the methylamino andethylamino groups;

dialkylamino groups in which each alkyl part is independently selectedfrom the group consisting of alkyl groups having from 1 to 4 carbonatoms, such as those exemplified above in relation to the dialkylaminogroups which may be represented by R¹ ;

alkanoylamino groups having from 1 to 5 carbon atoms, such as theformamido, acetamido, propionamido, butyramido, valerylamino andisovalerylamino groups, preferably the acetamido or propionamido group;

arylcarbonylamino groups in which the aryl part is as defined andexemplified above in relation to the aryl groups which may berepresented by R³ and R⁴ particularly the benzamido group;

and aryl groups as defined and exemplified above in relation to the arylgroups which may be represented by R³ and R⁴, particularly the phenylgroup.

Examples of substituents β are straight or branched chain alkyl groupshaving from 1 to 4 carbon atoms, and examples include the methyl, ethyl,propyl, isopropyl, butyl, isobutyl, sec-butyl and t-butyl groups,preferably the methyl, ethyl, propyl, isopropyl, butyl and sec-butylgroups, and most preferably the methyl or ethyl group.

Specific examples of such substituted and unsubstituted groups which maybe represented by R² are given hereafter.

Where R⁵ represents a substituted alkyl group, the alkyl moiety may be astraight or branched chain alkyl group having from 1 to 4 carbon atoms,and examples include the methyl, ethyl, propyl, isopropyl, butyl,isobutyl, sec-butyl and t-butyl groups, preferably the methyl, ethyl,propyl, isopropyl, butyl and sec-butyl groups, more preferably the ethylor propyl group having a substituent at the 2-position, and mostpreferably the ethyl group having a substituent at the 2-position. Thegroup is substituted by at least one, and preferably from 1 to 3, morepreferably 1, substituent selected from the group consisting ofsubstituents γ.

Examples of substituents γ include:

hydroxy groups;

alkanoyloxy groups having from 1 to 5 carbon atoms, such as the formoxy,acetoxy, propionyloxy, butyryloxy, valeryloxy and isovaleryloxy groups,preferably the acetoxy or propionyloxy group;

substituted alkanoyloxy groups which have from 2 to 5 carbon atoms andwhich are substituted by at least one substituent selected from thegroup consisting of substituents δ, such as the acetoxy, propionyloxy,butyryloxy, valeryloxy and isovaleryloxy groups, preferably the acetoxyor propionyloxy group; examples of substituents δ are:

carboxy groups;

alkoxycarbonyl groups in which the alkoxy part has from 1 to 4 carbonatoms, such as the methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl,isopropoxycarbonyl, butoxycarbonyl and isobutoxycarbonyl groups, ofwhich the methoxycarbonyl and ethoxycarbonyl groups are preferred;

aryloxycarbonyl groups in which the aryl part is as defined andexemplified above in relation to the aryl groups which may berepresented by R³ and R⁴, particularly the phenoxycarbonyl group; and

aryl groups as defined and exemplified above in relation to the arylgroups which may be represented by R³ and R⁴, particularly the phenylgroup;

especially, propionyloxy groups substituted at the 3-position by acarboxy, alkoxycarbonyl or aryloxycarbonyl group and acetoxy groupssubstituted by an aryl group;

arylcarbonyloxy groups in which the aryl part is as defined andexemplified above in relation to the aryl groups which may berepresented by R³ and R⁴ particularly the benzoyloxy group;

and cycloalkylcarbonyloxy groups in which the cycloalkyl part has from 3to 6 ring carbon atoms,, such as the cyclopropylcarbonyloxy,cyclobutylcarbonyloxy, cyclopentylcarbonyloxy and cyclohexylcarbonyloxygroups, which may be substituted or unsubstituted (preferablyunsubstituted) and, if substituted, have one or more substituentsselected from the group consisting of substituents α, preferably alkylgroups or alkoxy groups, as exemplified above, and more preferablymethyl or ethyl groups; the cycloalkylcarbonyloxy group is preferably acyclopentylcarbonyloxy or cyclohexylcarbonyloxy group.

Where R⁵ represents an aromatic heterocyclic group, this has 5 or 6 ringatoms, of which from 1 to 4 are hetero-atoms selected from the groupconsisting of oxygen, nitrogen and sulfur atoms. Where there is only onehetero-atom, this may be any of the oxygen, nitrogen and sulfur atoms.However, where there are two, three or four hetero-atoms, it ispreferred that 0 or 1 is an oxygen or sulfur atom and, where there areno oxygen or sulfur atoms, 1, 2, 3 or 4 are nitrogen atoms, or, wherethere is 1 oxygen or sulfur atom, 0, 1, 2 or 3 are nitrogen atoms.Examples of such groups include the furyl, thienyl, pyrrolyl, oxazolyl,isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, 1,2,3-,1,2,4-, 1,2,5- or 1,3,4-oxadiazolyl, 1,2,3-, 1,2,4-, 1,2,5- or1,3,4-thiadiazolyl, 1,2,3- or 1,2,4-triazolyl, tetrazolyl, pyridyl,pyrimidinyl, pyridazinyl, pyrazinyl and 1,2,3-, 1,2,4- or1,3,5-triazinyl groups. Of these, we prefer the imidazolyl,1,3,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-triazolyl, tetrazolyl,pyridyl and pyrimidinyl groups, more preferably the 1,3,4-oxadiazolyl,1,2,4-triazolyl, tetrazolyl and pyrimidinyl groups and most preferablythe 1,3,4-oxadiazolyl, 1,2,4-triazolyl and pyrimidinyl groups. Suchgroups may be unsubstituted or they may have one or more (preferablyfrom 1 to 3) substituents selected from the group consisting ofsubstituents α, in the case of substituents on carbon atoms, orsubstituents ε, in the case of substituents on nitrogen atoms. Examplesof substituents α have been given above. Examples of substituents ε areas follows:

alkyl groups having from 1 to 4 carbon atoms, such as those exemplifiedabove in relation to substituents β; and

hydroxyalkyl groups having from 2 to 4 carbon atoms, such as the2-hydroxyethyl, 2-hydroxypropyl, 3-hydroxypropyl, 2-hydroxybutyl,3-hydroxybutyl and 4-hydroxybutyl groups; preferably a 2-hydroxyethyl or3-hydroxypropyl group.

Specific examples of such substituted and unsubstituted groups which maybe represented by R⁵ are given hereafter.

B can represent an alkylene or alkylidene group having from 1 to 6carbon atoms. Examples include the methylene, ethylene, trimethylene,propylene, tetramethylene, 2-methyltrimethylene, pentamethylene andhexamethylene groups. Of these, we prefer the methylene, ethylene ortrimethylene group, more preferably a methylene or trimethylene group.

Preferably m is 0 or 1, and most preferably m is 0.

Preferably A is a group of formula --CH═CH-- or --CH₂ CH₂ --, and mostpreferably A is a group of formula --CH═CH--.

Specific examples of preferred optionally substituted 5-memberedaromatic heterocyclic groups containing from 1 to 3 hetero-atomsselected from the group consisting of oxygen, nitrogen and sulfur atoms,which may be represented by R² include the 2-furyl, 3-furyl,3-methyl-2-furyl, 4-methyl-2-furyl, 5-methyl-2-furyl, 2-methyl-3-furyl,4-methyl-3-furyl, 5-methyl-3-furyl, 5-chloro-2ofuryl, 5-chloro-3-furyl,3-amino-2furyl, 5-amino-2-furyl, 3-acetamido-2-furyl,5-acetamido-2-furyl, 5-phenyl-2-furyl, 5-(4-methylphenyl)-2furyl,5-(4-chlorophenyl)-2-furyl, 2,4-dimethyl-3-furyl, 2,5-dimethyl-3-furyl,3-methyl-5-amino-2-furyl, 2-thienyl, 3-thienyl, 3-methyl-2-thienyl,4-methyl-2-thienyl, 5-methyl-2-thienyl, 2-methyl-3-thienyl,4-methyl-3-thienyl, 5-methyl-3-thienyl, 5-ethyl-2-thienyl,4-methoxy-2-thienyl, 4-methoxy-3-thienyl, 4-hydroxy-2-thienyl,4-hydroxy-3-thienyl, 5-chloro-2-thienyl, 5-chloro-3 -thienyl,5-bromo-3-thienyl, 3-amino-2-thienyl, 5-amino- 2-thienyl,2-amino-3-thienyl, 4-amino-3-thienyl, 3-acetamido-2-thienyl,5-acetamido-2-thienyl, 2-acetamido-3-thienyl, 4-acetamido-3-thienyl,5-phenyl-2-thienyl, 5-(4-methylphenyl)-2-thienyl,5-(4-chlorophenyl)-2-thienyl, 3,4-dimethyl-2-thienyl,3,5-dimethyl-2-thienyl, 4,5-dimethyl-2-thienyl, 2,4-dimethyl-3-thienyl,2,5-dimethyl-3-thienyl, 4,5-dimethyl-3-thienyl,5-methyl-2-amino-3-thienyl, 4-methyl-5-chloro-3-thienyl,4,5-dichloro-2-thienyl, 2-amino-5-phenyl-3-thienyl,2,4,5-trimethyl-3-thienyl, 2,5-dimethyl-4-amino-3-thienyl, 2-pyrrolyl,3-pyrrolyl, 1-methyl-2-pyrrolyl, 3-methyl-2-pyrrolyl,4-methyl-2-pyrrolyl, 5-methyl-2-pyrrolyl, 1-methyl-3-pyrrolyl,2-methyl-3-pyrrolyl, 4-methyl-3-pyrrolyl, 5-methyl-3-pyrrolyl,4-methoxy-3-pyrrolyl, 4-hydroxy-3-pyrrolyl, 5-chloro-2-pyrrolyl,5-chloro-3-pyrrolyl, 3-amino-2-pyrrolyl, 4-amino-2-pyrrolyl,3-acetamido-2-pyrrolyl, 4-acetamido-2-pyrrolyl, 4-phenyl-2-pyrrolyl,5-phenyl-2-pyrrolyl, 5-phenyl-3-pyrrolyl, 4-(4-methylphenyl)-2-pyrrolyl,5-(4-methylphenyl)-2-pyrrolyl, 4-(4-methoxy-phenyl)-2-pyrrolyl,5-(4-methoxyphenyl)-2-pyrrolyl, 4-(4-fluorophenyl)-2-pyrrolyl,5-(4-fluorophenyl)-2pyrrolyl, 4-(4-chlorophenyl)-2-pyrrolyl,5-(4-chlorophenyl)-2-pyrrolyl, 5-(4-methylphenyl)-3-pyrrolyl,5-(4-methoxyphenyl)-3-pyrrolyl, 5-(4-fluorophenyl)-3-pyrrolyl,5-(4-chlorophenyI)-3-pyrrolyl, 1,3-dimethyl-2-pyrrolyl,1,4-dimethyl-2-pyrrolyl, 1,5-dimethyl-2-pyrrolyl,3,4-dimethyl-2-pyrrolyl, 3,5-dimethyl-2-pyrrolyl,4,5-dimethyl-2-pyrrolyl, 1,5-dimethyl-3-pyrrolyl,2,4-dimethyl-3-pyrrolyl, 2,5-dimethyl-3-pyrrolyl,1-methyl-4-hydroxy-3-pyrrolyl, 1-methyl-4-methoxy-3-pyrrolyl,1-methyl-2-chloro-3-pyrrolyl, 4-methyl-5-chloro-3-pyrrolyl,1-methyl-5-amino-2-pyrrolyl, 3,4,5-trimethyl-2-pyrrolyl,1,2,4-trimethyl-3-pyrrolyl, 1,4-dimethyl-5-chloro-3-pyrrolyl,1,4-dimethyl-5-bromo-3 -pyrrolyl, 3,5-dimethyl-4-amino-2-pyrrolyl,2-oxazolyl , 4-oxazolyl, 5-oxazolyl, 2-methyl-4-oxazolyl,5-methyl-2-oxazolyl, 2-methoxy-4-oxazolyl, 2-hydroxy-4-oxazolyl,2-phenyl-4-oxazolyl, 5-phenyl-2-oxazolyl, 2,5-dimethyl-4-oxazolyl,2,4-dimethyl-5-oxazolyl, 5-methyl-2-phenyl-4-oxazolyl,4-methyl-2-phenyl-5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl,3-methyl-4-isoxazolyl, 4-methyl-3-isoxazolyl, 5-methyl-3-isoxazolyl,3-methoxy-4-isoxazolyl, 4-methoxy-3-isoxazolyl, 3-hydroxy-4-isoxazolyl,3-hydroxy-5-isoxazolyl, 4-hydroxy-3-isoxazolyl, 5-amino-4-isoxazolyl,4-amino-3-isoxazolyl, 4-phenyl-3-isoxazolyl, 5-phenyl-3-isoxazolyl,4-(4-methylphenyl)-3-isoxazolyl, 5-(4-methylphenyl)-3-isoxazolyl,4,5-dimethyl-3-isoxazolyl, 5-methyl-4-hydroxy-3-isoxazolyl, 2-thiazolyl,4-thiazolyl, 5-thiazolyl, 4-methyl-2-thiazolyl, 5-methyl-2-thiazolyl,2-methyl-4-thiazolyl, 5-methyl-4-thiazolyl, 2-methyl-5-thiazolyl,4-methyl-5-thiazolyl, 2-methoxy-4-thiazolyl, 2-methoxy-5-thiazolyl,2-hydroxy-4-thiazolyl, 2-hydroxy-5-thiazolyl, 5-chloro-2-thiazolyl,2-chloro-4-thiazolyl, 5-chloro-4-thiazolyl, 2-chloro-5-thiazolyl,4-chloro-5thiazolyl, 2-amino-4-thiazolyl, 5-amino-4-thiazolyl,2-amino-5-thiazolyl, 2-acetamido-4-thiazolyl, 5-acetamido-4-thiazolyl,2-acetamido-5-thiazolyl, 2-phenyl-4-thiazolyl, 2-phenyl-5-thiazolyl,4,5-dimethyl-2-thiazolyl, 2,5-dimethyl-4-thiazolyl,2,4-dimethyl-5-thiazolyl, 5-methyl-2-hydroxy-4-thiazolyl,4-methyl-2-hydroxy-5-thiazolyl, 5-methyl-2-chloro-4-thiazolyl,4-methyl-2-chloro-5-thiazolyl, 2-methyl-4-chloro-5-thiazolyl,5-methyl-2-amino-4-thiazolyl, 2-methyl-5-amino-4-thiazolyl,4-methyl-2-amino-5-thiazolyl, 3-isothiazolyl, 4-isothiazolyl,3-pyrazolyl, 4-pyrazolyl, 1-methyl-4-pyrazolyl, 3-methyl-4-pyrazolyl,1-methyl-3-pyrazolyl, 4-methyl-3-pyrazolyl, 5-methyl-3-pyrazolyl,1-methyl-5-pyrazolyl, 1-ethyl-4-pyrazolyl, 1-ethyl-3-pyrazolyl,5-ethyl-3-pyrazolyl, 1-propyl-4-pyrazolyl, 1-propyl-3-pyrazolyl,5-propyl-3-pyrazolyl, 1-butyl-4-pyrazolyl, 4-methoxy-3-pyrazolyl,4-propoxy-3-pyrazolyl, 4-hydroxy-3-pyrazolyl, 4-chloro-3pyrazolyl,3-chloro-4-pyrazolyl, 4-bromo-3-pyrazolyl, 4-amino-3-pyrazolyl,5-amino-3-pyrazolyl, 3-amino-4-pyrazolyl, 3-acetamido-4-pyrazolyl,3-propionylamino-4-pyrazolyl, 4-acetamido-3-pyrazolyl,5-acetamido-3-pyrazolyl, 5-phenyl-3-pyrazolyl, 1,3-dimethyl-4-pyrazolyl,1,5-dimethyl-4-pyrazolyl, 3,5-dimethyl-4-pyrazolyl,1,4-dimethyl-3-pyrazolyl, 1,5-dimethyl-3-pyrazolyl,4,5-dimethyl-3-pyrazolyl, 1,3-dimethyl-5-pyrazolyl,1,4-dimethyl-5-pyrazolyl, 1-methyl-4-methoxy-3-pyrazolyl,5-methyl-4-hydroxy-3-pyrazolyl, 1-methyl-3-chloro-4-pyrazolyl,1-methyl-5-chloro-4-pyrazolyl, 5-methyl-3-chloro-4-pyrazolyl,1-methyl-4-chloro-3-pyrazolyl, 5-methyl-4-chloro-3-pyrazolyl,1-methyl-4-chloro-5-pyrazolyl, 1-methyl-3-amino-4-pyrazolyl,1-methyl-5-amino-4-pyrazolyl, 5-methyl-3-amino-4-pyrazolyl,1-methyl-3-acetamido-4-pyrazolyl, 1-methyl-5-acetamido-4-pyrazolyl,3-methyl-5-acetamido-4-pyrazolyl, 1-methyl-5-amino-3-pyrazolyl,5-methyl-4-amino-3-pyrazolyl, 4-methyl-5-amino-3-pyrazolyl,1,3,5-trimethyl-4-pyrazolyl, 1,4,5-trimethyl-3-pyrazolyl,1,3,4-trimethyl-5-pyrazolyl, 1,3-dimethyl-4-chloro-5-pyrazolyl,2-imidazolyl, 4-imidazolyl, 1-methyl-2-imidazolyl,5-methyl-2-imidazolyl, 1-methyl-4-imidazolyl, 2-methyl-4-imidazolyl,5-methyl-4-imidazolyl, 1,2,3-oxadiazol-4-yl, 1,2,3-oxadiazol-5-yl,5-methyl-1,2,3-oxadiazol-4-yl, 4-methyl-1,2,3-oxadiazol-5-yl,1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 1,2,5-oxodiazol-3-yl,4-methyl-1,2,5-oxadiazol-3-yl, 4-phenyl-1,2,5-oxadiazol-3-yl,4-(4-methylphenyl)-1,2,5-oxadiazol-3-yl, 1,3,4-oxadiazol-2-yl,1,2,3-thiadiazol-4-yl, 1,2,3-thiadiazol-5-yl,5-methyl-1,2,3-thiadiazol-4-yl, 5-phenyl-1,2,3-thiadiazol-4-yl,5-(4-methyl-phenyl)-1,2,3-thiadiazol-4-yl,4-methyl-1,2,3-thiadiazol-5-yl, 1,2,4-thiadiazol-3-yl,1,2,4-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl,4-methyl-1,2,5-thiadiazol-3-yl, 1,3,4-thiadiazol-2-yl,1,2,3-triazol-4-yl, 1-methyl-1,2,3-triazol-4-yl,5-methyl-1,2,3-triazol-4-yl, 1,5-dimethyl-1,2,3-triazol-4-yl,1,2,4-triazol-5-yl, 1-methyl-1,2,4-triazol-3-yl and2-ethyl-4-methyl-1,2,3-triazol-5-yl groups.

Examples of more preferred such groups include: the 2-furyl, 3-furyl,3-methyl-2-furyl, 4-methyl-2-furyl, 5-methyl-2-furyl, 2- methyl-3-furyl,4-methyl-3-furyl, 5-methyl-3-furyl, 2- thienyl, 3-thienyl,3-methyl-2-thienyl, 4-methyl-2- thienyl, 5-methyl-2-thienyl,2-methyl-3-thienyl, 4-methyl-3-thienyl, 5-methyl-3-thienyl,5-chloro-2-thienyl, 5-chloro-3-thienyl, 3-amino-2-thienyl,5-amino-2-thienyl, 2-amino-3-thienyl, 4-amino-3-thienyl,3-acetamido-2-thienyl, 5-acetamido-2-thienyl, 2-acetamido-3-thienyl,4-acetamido-3-thienyl, 2-pyrrolyl, 3-pyrrolyl, 1-methyl-2-pyrrolyl,3-methyl-2-pyrrolyl, 4-methyl-2-pyrrolyl, 5-methyl-2-pyrrolyl,1-methyl-3-pyrrolyl, 2-methyl-3-pyrrolyl, 4-methyl-3-pyrrolyl,5-methyl-3-pyrrolyl, 4-methoxy-3-pyrrolyl, 5-chloro-2-pyrrolyl,5-chloro-3-pyrrolyl, 3-amino-2-pyrrolyl, 4-amino-2-pyrrolyl, 2-oxazolyl,4-oxazolyl, 5-oxazolyl, 2-methyl-4-oxazolyl, 3-isoxazolyl, 4-isoxazolyl,3-methyl-4-isoxazolyl, 4-methyl-3-isoxazolyl, 5-methyl-3-isoxazolyl,2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 4-methyl-2-thiazolyl,5-methyl-2-thiazolyl, 2-methyl-4-thiazolyl, 5-methyl-4-thiazolyl,2-methyl-5-thiazolyl, 4-methyl-5-thiazolyl, 2-chloro-4-thiazolyl,5-chloro-4-thiazolyl, 2-chloro-5-thiazolyl, 4-chloro-5-thiazolyl,2-amino-4-thiazolyl, 5-amino-4-thiazolyl, 3-pyrazolyl, 4-pyrazolyl,1-methyl-4-pyrazolyl, 3-methyl-4-pyrazolyl, 1-methyl-3-pyrazolyl,4-methyl-3-pyrazolyl, 5-methyl-3-pyrazolyl, 1-methyl-5-pyrazolyl,1-ethyl-4-pyrazolyl, 4-methoxy-3-pyrazolyl, 4-chloro-3-pyrazolyl,3-chloro-4-pyrazolyl, 4-amino-3-pyrazolyl, 5-amino-3-pyrazolyl,3-amino-4-pyrazolyl, 3-acetamido-4-pyrazolyl, 2-imidazolyl,4-imidazolyl, 1-methyl-2-imidazolyl, 5-methyl-2-imidazolyl,1-methyl-4-imidazolyl, 2-methyl-4-imidazolyl, 5-methyl-4-imidazolyl,1,2,3-thiadiazol-4-yl, 1,2,3-thiadiazol-5-yl,5-methyl-1,2,3-thiadiazol-4-yl, 4-methyl-1,2,3-thiadiazol-5-yl,1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl,4-methyl-1,2,5-thiadiazol-3-yl and 1,3,4-thiadiazol-2-yl groups.

Examples of still more preferred such groups include: the 2-furyl,3-furyl, 2-thienyl, 3-thienyl, 3-methyl-2-thienyl, 4-methyl-2-thienyl,5-methyl-2-thienyl, 2-methyl-3-thienyl, 4-methyl-3-thienyl,5-methyl-3-thienyl, 5-chloro-2-thienyl, 5-chloro-3-thienyl, 2-pyrrolyl,3-pyrrolyl, 1-methyl-2-pyrrolyl, 3-methyl-2-pyrrolyl,4-methyl-2-pyrrolyl, 5-methyl-2-pyrrolyl, 1-methyl-3-pyrrolyl,2-methyl-3-pyrrolyl, 4-methyl-3-pyrrolyl, 5-methyl-3-pyrrolyl,2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl,2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 2-methyl-4-thiazolyl,5-methyl-4-thiazolyl, 2-methyl-5-thiazolyl, 4-methyl-5-thiazolyl,3-pyrazolyl, 4-pyrazolyl, 1-methyl-4-pyrazolyl, 3-methyl-4-pyrazolyl,1-methyl-3-pyrazolyl, 4-methyl -3-pyrazolyl, 5-methyl-3-pyrazolyl,1-methyl-5-pyrazolyl, 3-chloro-4-pyrazolyl, 4-amino-3-pyrazolyl,5-amino-3-pyrazolyl, 3-amino-4-pyrazolyl, 2-imidazolyl, 4-imidazolyl,1,2,3-thiadiazol-4-yl 1,2,3-thiadiazol-5-yl, 1,2,4-thiadiazol-3-yl and1,2,4-thiadiazol-5-yl.

Examples of the most preferred such groups which may be represented byR² include: the 2-thienyl, 3-thienyl, 5-methyl-2-thienyl,5-chloro-3-thienyl, 2-pyrrolyl, 3-pyrrolyl, 1-methyl-2-pyrrolyl,2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 3-pyrazolyl, 4-pyrazolyl,1-methyl-4-pyrazolyl, 3-methyl-4-pyrazolyl, 5-methyl-3-pyrazolyl,3-amino-4-pyrazolyl, 1,2,3-thiadiazol-4-yl groups and1,2,3-thiadiazol-5-yl groups.

Specific examples of optionally substituted 5- or 6-membered aromaticheterocyclic groups having from 1 to 4 hetero-atoms selected from thegroup consisting of oxygen, nitrogen and sulfur atoms, which may berepresented by R⁵ include: the 2-furyl, 3-furyl, 3-methyl-2-furyl,4-methyl-2-furyl, 5-methyl-2-furyl, 2-methyl-3-furyl, 4-methyl-3-furyl,5-methyl-3-furyl, 5-chloro-2-furyl, 5-chloro-3-furyl, 3-amino-2-furyl,5-amino-2-furyl, 3-acetamido-2-furyl, 5-acetamido-2-furyl,5-phenyl-2-furyl, 5-(4-methylphenyl)-2-furyl,5-(4-chlorophenyl)-2-furyl, 2,4-dimethyl-3-furyl, 2,5-dimethyl-3-furyl,3-methyl-5-amino-2-furyl, 2-thienyl, 3-thienyl, 3-methyl-2-thienyl,4-methyl-2-thienyl, 5-methyl-2-thienyl, 2-methyl-3-thienyl,4-methyl-3-thienyl, 5-methyl-3-thienyl, 5-ethyl-2-thienyl,4-methoxy-2-thienyl, 4-methoxy-3-thienyl, 4-hydroxy-2-thienyl,4-hydroxy-3-thienyl, 5-chloro-2-thienyl, 5-chloro-3-thienyl,5-bromo-3-thienyl, 3-amino-thienyl, 5-amino-2-thienyl,2-amino-3-thienyl, 4-amino-3-thienyl, 3-acetamido-2-thienyl,5-acetamido-2-thienyl, 2-acetamido-3-thienyl, 4-acetamido-3-thienyl,5-phenyl-2-thienyl, 5-(4-methylphenyl)-2-thienyl,5-(4-chlorophenyl)-2-thienyl, 3,4-dimethyl-2-thienyl,3,5-dimethyl-2-thienyl, 4,5-dimethyl-2-thienyl, 2,4-dimethyl-3-thienyl,2,5-dimethyl-3-thienyl, 4,5-dimethyl-3-thienyl,5-methyl-2-amino-3-thienyl, 4-methyl-5-chloro-3-thienyl,4,5-dichloro-2-thienyl, 2-amino-5-phenyl-3-thienyl,2,4,5-trimethyl-3-thienyl, 2,5-dimethyl-4-amino-3-thienyl, 2-pyrrolyl,3-pyrrolyl, 1-methyl-2-pyrrolyl, 3-methyl-2-pyrrolyl,4-methyl-2-pyrrolyl, 5-methyl-2-pyrrolyl, 1-methyl-3-pyrrolyl,2-methyl-3-pyrrolyl, 4-methyl-3-pyrrolyl, 5-methyl-3-pyrrolyl,4-methoxy-3-pyrrolyl, 4-hydroxy-3-pyrrolyl, 5-chloro-2-pyrrolyl,5-chloro-3-pyrrolyl, 3-amino-2-pyrrolyl, 4-amino-2-pyrrolyl,3-acetamido-2-pyrrolyl, 4-acetamido-2-pyrrolyl, 4-phenyl-2-pyrrolyl,5-phenyl-2-pyrrolyl, 5-phenyl-3-pyrrolyl, 4-(4-methylphenyl)-2-pyrrolyl,5-(4-methylphenyl)-2-pyrrolyl, 4-(4-methoxyphenyl)-2-pyrrolyl,5-(4-methoxyphenyl)-2-pyrrolyl, 4-(4-fluorophenyl)-2-pyrrolyl,5-(4-fluorophenyl)-2-pyrrolyl, 4-(4-chlorophenyl)-2-pyrrolyl,5-(4-chlorophenyl)-2-pyrrolyl, 5-(4-methylphenyl)-3-pyrrolyl,5-(4-methoxyphenyl)-3-pyrrolyl, 5-(4-fluorophenyl)-3-pyrrolyl,5-(4-chlorophenyl)-3-pyrrolyl, 1-(2-hydroxyethyl)-2-pyrrolyl,1-(3-hydroxypropyl)-2-pyrrolyl, 1-(2-hydroxyethyl)-3-pyrrolyl,1-(3-hydroxypropyl)-3-pyrrolyl, 1,3-dimethyl-2-pyrrolyl,1,4-dimethyl-2-pyrrolyl, pyrrolyl, 1,5-dimethyl-2-pyrrolyl,3,4-dimethyl-2-pyrrolyl, 3,5-dimethyl-2-pyrrolyl,4,5-dimethyl-2-pyrrolyl, 1,5-dimethyl-3-pyrrolyl,2,4-dimethyl-3-pyrrolyl, 2,5-dimethyl-3-pyrrolyl,1-methyl-4-hydroxy-3-pyrrolyl, 1-methyl-4-methoxy-3-pyrrolyl,1-methyl-2-chloro-3-pyrrolyl, 4-methyl-5-chloro-3-pyrrolyl,1-methyl-5-amino-2-pyrrolyl, 3,4,5-trimethyl-2-pyrrolyl,1,2,4-trimethyl-3-pyrrolyl, 1,4-dimethyl-5-chloro-3-pyrrolyl,1,4-dimethyl-5-bromo-3-pyrrolyl, 3,5-dimethyl-4-amino-2-pyrrolyl,2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 2-methyl-4-oxazolyl,5-methyl-2-oxazolyl, 2-methoxy-4-oxazolyl, 2-hydroxy-4-oxazolyl,2-phenyl-4-oxazolyl, 5-phenyl-2-oxazolyl, 2,5-dimethyl-4-oxazolyl,2,4-dimethyl-5-oxazolyl, 5-methyl-2-phenyl-4-oxazolyl,4-methyl-2-phenyl-5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl,3-methyl-4-isoxazolyl, 4-methyl-3-isoxazolyl, 5-methyl-3-isoxazolyl,3-methoxy-4-isoxazolyl, 4-methoxy-3-isoxazolyl, 3-hydroxy-4-isoxazolyl,3-hydroxy-5-isoxazolyl, 4-hydroxy-3-isoxazolyl, 5-amino-4-isoxazolyl,4-amino-3-isoxazolyl, 4-phenyl-3-isoxazolyl, 5-phenyl-3-isoxazolyl,4-(4-methylphenyl)-3-isoxazolyl, 5-(4-methylphenyl)-3-isoxazolyl,4,5-dimethyl-3-isoxazolyl, 5-methyl-4-hydroxy-3-isoxazolyl, 2-thiazolyl,4-thiazolyl, 5-thiazolyl, 4-methyl-2-thiazolyl, 5-methyl-2-thiazolyl,2-methyl-4-thiazolyl, 5-methyl-4-thiazolyl, 2-methyl-5-thiazolyl,4-methyl-5-thiazolyl, 2-methoxy-4-thiazolyl, 2-methoxy-5-thiazolyl,2-hydroxy-4-thiazolyl, 2-hydroxy-5-thiazolyl, 5-chloro-2-thiazolyl,2-chloro-4-thiazolyl, 5-chloro-4-thiazolyl, 2-chloro-5-thiazolyl,4-chloro-5-thiazolyl, 2-amino-4-thiazolyl, 5-amino-4-thiazolyl,2-amino-5-thiazolyl, 2-acetamido-4-thiazolyl, 5-acetamido-4-thiazolyl,2-acetamido-5-thiazolyl, 2-phenyl-4-thiazolyl, 2-phenyl-5-thiazolyl,4,5-dimethyl-2-thiazolyl, 2,5-dimethyl-4-thiazolyl,2,4-dimethyl-5-thiazolyl, 5-methyl-2-hydroxy-4-thiazolyl,4-methyl-2-hydroxy-5-thiazolyl, 5-methyl-2-chloro-4-thiazolyl,4-methyl-2-chloro-5-thiazolyl, 2-methyl-4-chloro-5-thiazolyl,5-methyl-2-amino-4-thiazolyl, 2-methyl-5-amino-4-thiazolyl,4-methyl-2-amino-5-thiazolyl, 3-isothiazolyl, 4-isothiazolyl,3-pyrazolyl, 4-pyrazolyl, 1-methyl-4-pyrazolyl, 3-methyl-4-pyrazolyl,1-methyl-3-pyrazolyl, 4-methyl-3-pyrazolyl, 5-methyl-3-pyrazolyl,1-methyl-5-pyrazolyl, 1-ethyl-4-pyrazolyl, 1-ethyl-3-pyrazolyl,5-ethyl-3-pyrazolyl, 1-propyl-4-pyrazolyl, 1-propyl-3-pyrazolyl,5-propyl-3-pyrazolyl, 1-butyl-4-pyrazolyl, 4-methoxy-3-pyrazolyl,4-propoxy-3-pyrazolyl, 4-hydroxy-3-pyrazolyl, 4-chloro-3-pyrazolyl,3-chloro-4-pyrazolyl, 4-bromo-3-pyrazolyl, 4-amino-3-pyrazolyl,5-amino-3-pyrazolyl, 3-amino-4-pyrazolyl, 3-acetamido-4-pyrazolyl,3-propionylamino-4-pyrazolyl, 4-acetamido-3-pyrazo lyl,5-acetamido-3-pyrazolyl, 5-phenyl-3-pyrazolyl ,1-(2-hydroxyethyl)-3-pyrazolyl, 1-(3-hydroxypropyl)- 3-pyrazolyl,1-(2-hydroxyethyl)-4-pyrazolyl, 1-(3-hydroxypropyl)-4-pyrazolyl,1-(2-hydroxyethyl)-5-pyrazolyl, 1-(3-hydroxypropyl)-5-pyrazolyl,1,3-dimethyl-4-pyrazolyl, 1,5-dimethyl-4-pyrazolyl,3,5-dimethyl-4-pyrazolyl, 1,4-dimethyl-3-pyrazolyl,1,5-dimethyl-3-pyrazolyl, 4,5-dimethyl-3-pyrazolyl,1,3-dimethyl-5-pyrazolyl, 1,4-dimethyl-5-pyrazolyl,1-methyl-4-methoxy-3-pyrazolyl, 5-methyl-4-hydroxy-3-pyrazolyl,1-methyl-3-chloro-4-pyrazolyl, 1-methyl-5-chloro-4-pyrazolyl,5-methyl-3-chloro-4-pyrazolyl, 1-methyl-4-chloro-3-pyrazolyl,5-methyl-4-chloro-3-pyrazolyl, 1-methyl-4-chloro-5-pyrazolyl,1-methyl-3-amino-4-pyrazolyl, 1-methyl-5-amino-4-pyrazolyl,5-methyl-3-amino-4-pyrazolyl, 1-methyl-3-acetamido-4-pyrazolyl,1-methyl-5-acetamido-4-pyrazolyl, 3-methyl-5-acetamido-4-pyrazolyl,1-methyl-5-amino-3-pyrazolyl, 5-methyl-4-amino-3-pyrazolyl,4-methyl-5-amino-3-pyrazolyl, 1,3,5-trimethyl-4-pyrazolyl,1,4,5-trimethyl-3-pyrazolyl, 1,3,4-trimethyl-5-pyrazolyl,1,3-dimethyl-4-chloro-5-pyrazolyl, 2-imidazolyl, 4-imidazolyl,1-methyl-2-imidazolyl, 5-methyl-2-imidazolyl, 1-methyl-4-imidazolyl,2-methyl-4-imidazolyl, 5-methyl-4-imidazolyl, 1-ethyl-2-imidazolyl,4-ethyl-2-imidazolyl, 1-(2-hydroxyethyl)-2-imidazolyl,1-(3-hydroxypropyl)-2-imidazolyl, 4-amino-2-imidazolyl,2-amino-4-imidazolyl, 5-amino-4-imidazolyl, 4-chloro-2-imidazolyl,2-chloro-4-imidazolyl, 5-chloro-4-imidazolyl, 1,2,3-oxadiazol-4-yl,1,2,3-oxadiazol-5-yl, 5-methyl-1,2,3-oxadiazol-4-yl,4-methyl-1,2,3-oxadiazol-5-yl, 1,2,4-oxadiazol-3-yl,1,2,4-oxadiazol-5-yl, 1,2,5-oxadiazol-3-yl,4-methyl-1,2,5-oxadiazol-3-yl, 4-phenyl-1,2,5-oxadiazol-3-yl,4-(4-methylphenyl)-1,2,5-oxadiazol-3-yl, 1,3,4-oxadiazol-2-yl,5-methyl-1,3,4-oxadiazol-2-yl, 5-ethyl-1,3,4-oxadiazol-2-yl,5-phenyl-1,3,4-oxadiazol-2-yl, 5-chloro-1,3,4-oxadiazol-2-yl,5-amino-1,3,4-oxadiazol-2-yl, 5-acetamido-1,3,4-oxadiazol-2-yl,1,2,3-thiadiazol-4-yl, 1,2,3-thiadiazol-5-yl,5-methyl-1,2,3-thiadiazol-4-yl, 5-phenyl-1,2,3-thiadiazol-4-yl,5-(4-methylphenyl)-1,2,3-thiadiazol-4-yl,4-methyl-1,2,3-thiadiazol-5-yl, 1,2,4-thiadiazol-3-yl,1,2,4-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl,4-methyl-1,2,5-thiadiazol-3-yl, 1,3,4-thiadiazol-2-yl,5-methyl-1,3,4-thiadiazol-2-yl, 5-ethyl-1,3,4-thiadiazol-2-yl,5-phenyl-1,3,4-thiadiazol-2-yl, 5-chloro-1,3,4-thiadiazol-2-yl,5-amino-1,3,4-thiadiazol-2-yl, 5-acetamido-1,3,4-thiadiazol-2-yl,1,2,3-triazol-4-yl, 1-methyl-1,2,3-triazol-4-yl,5-methyl-1,2,3-triazol-4-yl, 1,5-dimethyl-1,2,3-triazol-4-yl,1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, 1-methyl-1,2,4-triazol-3-yl,1-methyl-1,2,4-triazol-5-yl, 5-methyl-1,2,4-triazol-3-yl,5-ethyl-1,2,4-triazol-3-yl, 5-phenyl-1,2,4-triazol-3-yl,1-(2-hydroxyethyl)-1,2,4-triazol-3-yl,1-(3-hydroxypropyl)-1,2,4-triazol-3-yl,1-(2-hydroxyethyl)-1,2,4-triazol-5-yl,1-(3-hydroxypropyl)-1,2,4-triazol-5-yl, 5-chloro-1,2,4-triazol-3-yl,5-amino-1,2,4-triazol-3-yl, 5-acetamido-1,2,4-triazol-3-yl,1,3-dimethyl-1,2,4-triazol-5-yl, 1,5-dimethyl-1,2,4-triazol-3-yl,2-ethyl-4-methyl-1,2,3-triazol-5-yl, tetrazol-5-yl,1-methyltetrazol-5-yl, 2-methyltetrazol-5-yl, 1-ethyltetrazol-5-yl,2-ethyltetrazol-5-yl, 1-phenyltetrazol-5-yl, 2-phenyltetrazol-5-yl,1-(2-hydroxyethyl)tetrazol-5-yl, 2-(2-hydroxyethyl)-tetrazol-5-yl,1-(2-hydroxypropyl) tetrazol-5-yl, 2-(2-hydroxypropyl) tetrazol- 5-yl,1-(3 -hydroxypropyl)-tetrazol-5-yl, 2-(3-hydroxypropyl)tetrazol-5-yl,2-pyridyl, 3-pyridyl, 4-pyridyl, 3-methyl-2-pyridyl, 4-methyl-2-pyridyl,5-methyl-2-pyridyl, 6-methyl-2-pyridyl, 2-methyl-4-pyridyl,3-methyl-4-pyridyl, 3-chloro-2-pyridyl, 4-chloro-2-pyridyl,5-chloro-2-pyridyl, 6-chloro-2-pyridyl, 2-chloro-3-pyridyl,4-chloro-3-pyridyl, 5-chloro-3-pyridyl, 6-chloro-3-pyridyl,2-chloro-4-pyridyl, 3-chloro-4-pyridyl, 3-amino-2-pyridyl,4-amino-2-pyridyl, 5-amino-2-pyridyl, 6-amino-2-pyridyl,2-amino-3-pyridyl, 4-amino-3-pyridyl, 5-amino-3-pyridyl,6-amino-3-pyridyl, 2-amino-4-pyridyl, 3-amino-4-pyridyl,3-hydroxy-2-pyridyl, 4-hydroxy-2-pyridyl, 5-hydroxy-2-pyridyl,6-hydroxy-2-pyridyl, 2-hydroxy-4-pyridyl, 3-hydroxy-4-pyridyl,3-phenyl-2-pyridyl, 4-phenyl-2-pyridyl, 5-phenyl-2-pyridyl,6-phenyl-2-pyridyl, 2-phenyl-4-pyridyl, 3-phenyl-4-pyridyl,2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 4-methyl-2-pyrimidinyl,5-methyl-2-pyrimidinyl, 2-methyl-4-pyrimidinyl, 5-methyl-4-pyrimidinyl,6-methyl-4-pyrimidinyl, 2-methyl-5-pyrimidinyl, 4-methyl-5-pyrimidinyl,4-phenyl-2-pyrimidinyl, 5-phenyl-2-pyrimidinyl, 2-phenyl-4-pyrimidinyl,5-phenyl-4-pyrimidinyl, 6-phenyl-4-pyrimidinyl, 2-phenyl-5-pyrimidinyl,4-phenyl-5-pyrimidinyl, 4-chloro-2-pyrimidinyl, 5-chloro-2-pyrimidinyl,2-chloro-4-pyrimidinyl, 5-chloro-4-pyrimidinyl, 6-chloro-4-pyrimidinyl,2-chloro-5-pyrimidinyl, 4-chloro-5-pyrimidinyl, 4-amino-2-pyrimidinyl,5-amino-2-pyrimidinyl, 2-amino-4-pyrimidinyl, 5-amino-4-pyrimidinyl,6-amino-4-pyrimidinyl, 2-amino-5-pyrimidinyl, 4-amino-5-pyrimidinyl,4-acetamido-2-pyrimidinyl, 5-acetamido-2-pyrimidinyl,2-acetamido-4-pyrimidinyl, 5-acetamido-4-pyrimidinyl,6-acetamido-4-pyrimidinyl, 2-acetamido-5-pyrimidinyl,4-acetamido-5-pyrimidinyl, 4,5-dimethyl-2-pyrimidinyl,4,6-dimethyl-2-pyrimidinyl, 2,5-dimethyl-4-pyrimidinyl,2,6-dimethyl-4-pyrimidinyl, 2,4-dimethyl-5-pyrimidinyl,2,6-dimethyl-5-pyrimidinyl, 4-amino-5-hydroxy-2-pyrimidinyl,4-amino-6-hydroxy-2-pyrimidinyl, 2-amino-5-hydroxy-4-pyrimidinyl,2-amino-6-hydroxy-4-pyrimidinyl, 2-amino-4-hydroxy-5-pyrimidinyl,5-amino-2-hydroxy-4-pyrimidinyl, 6-amino-2-hydroxy-4-pyrimidinyl,4-amino-2-hydroxy-5-pyrimidinyl, 4,5-diamino-2-pyrimidinyl,4,6-diamino-2-pyrimidinyl, 5-diamino-4-pyrimidinyl,2,6-diamino-4-pyrimidinyl, 4-diamino-5-pyrimidinyl,2,6-diamino-5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl,4-methyl-3-pyridazinyl, 5-methyl-3-pyridazinyl, 6-methyl-3-pyridazinyl,3-methyl-4 -pyridazinyl, 5-methyl-4-pyridazinyl, 6-methyl-4-pyridazinyl, 4-chloro-3-pyridazinyl, 5-chloro-3 -pyridazinyl,6-chloro-3-pyridazinyl, 3-chloro-4 -pyridazinyl, 5-chloro-4-pyridazinyl,6-chloro-4 -pyridazinyl, 4-hydroxy-3-pyridazinyl,5-hydroxy-3-pyridazinyl, 6-hydroxy-3-pyridazinyl,3-hydroxy-4-pyridazinyl, 5-hydroxy-4-pyridazinyl,6-hydroxy-4-pyridazinyl, 4-amino-3-pyridazinyl, 5-amino-3-pyridazinyl,6-amino-3-pyridazinyl, 3-amino-4-pyridazinyl, 5-amino-4-pyridazinyl,6-amino-4-pyridazinyl, 2-pyrazinyl, 3-amino-2-pyrazinyl,5-amino-2-pyrazinyl, 6-amino-2-pyrazinyl, 3-hydroxy-2-pyrazinyl,5-hydroxy-2-pyrazinyl, 6-hydroxy-2-pyrazinyl, 3,5-dihydroxy-2-pyrazinyl,3,6-dihydroxy-2-pyrazinyl, 1,2,3-triazin-4-yl, 1,2,3-triazin-5-yl,5-methyl-1,2,3-triazin-4-yl, 6-methyl-1,2,3-triazin-4-yl,4-methyl-1,2,3-triazin-5-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl,1,2,4-triazin-6-yl, 5-methyl-1,2,4triazin-3-yl,6-methyl-1,2,4-triazin-3-yl, 3-methyl-1,2,4-triazin-5-yl,6-methyl-1,2,4-triazin-5-yl, 3-methyl-1,2,4-triazin-6-yl,5-methyl-1,2,4-triazin-6-yl, 1,3,5-triazin-2-yl and4-methyl-1,3,5-triazin-2-yl groups.

Examples of preferred such groups include: the 2-furyl, 3 -furyl,3-methyl-2-furyl, 4-methyl-2-furyl, 5-methyl-2 -furyl, 2-methyl-3-furyl,4-methyl-3-furyl, 5-methyl-3 -furyl, 2-thienyl, 3-thienyl,3-methyl-2-thienyl, 4 -methyl-2-thienyl, 5-methyl-2-thienyl, 2-methyl-3-thienyl, 4-methyl-3-thienyl, 5-methyl-3-thienyl, 5 -ethyl-2-thienyl,4-methoxy-2-thienyl, 4-methoxy- 3-thienyl, 3-amino-2-thienyl,5-amino-2-thienyl, 2-amino-3-thienyl, 4-amino-3-thienyl, 2-pyrrolyl,3-pyrrolyl, 1-methyl-2-pyrrolyl, 3-methyl-2-pyrrolyl,4-methyl-2-pyrrolyl, 5-methyl-2-pyrrolyl, 1-methyl-3-pyrrolyl,2-methyl-3-pyrrolyl, 4-methyl-3-pyrrolyl, 5-methyl-3-pyrrolyl,4-methoxy-3-pyrrolyl, 4-hydroxy-3-pyrrolyl, 5-chloro-2-pyrrolyl,5-chloro-3-pyrrolyl, 3-amino-2-pyrrolyl, 4-amino-2-pyrrolyl,3-acetamido-2-pyrrolyl, 4-acetamido-2-pyrrolyl, 4-phenyl-2-pyrrolyl,5-phenyl-2-pyrrolyl, 5-phenyl-3-pyrrolyl, 4-(4-methylphenyl)-2-pyrrolyl,5-(4-methylphenyl)-2-pyrrolyl, 4-(4-methoxyphenyl)-2-pyrrolyl,5-(4-methoxyphenyl)-2-pyrrolyl, 4-(4-chlorophenyl)-2-pyrrolyl,5-(4-chlorophenyl)-2-pyrrolyl, 5-(4-methylphenyl)-3-pyrrolyl,1-(2-hydroxyethyl)-2-pyrrolyl, 1-(3-hydroxypropyl)-2-pyrrolyl,1-(2-hydroxyethyl)-3-pyrrolyl, 1-(3-hydroxypropyl)-3-pyrrolyl,1,3-dimethyl-2-pyrrolyl, 1,4-dimethyl-2-pyrrolyl,1,5-dimethyl-2-pyrrolyl, 3,4-dimethyl-2-pyrrolyl,4,5-dimethyl-2-pyrrolyl, 1,5-dimethyl-3-pyrrolyl,2,4-dimethyl-3-pyrrolyl, 2,5-dimethyl-3-pyrrolyl, 2-oxazolyl,4-oxazolyl, 5-oxazolyl, 2-methyl-4-oxazolyl, 5-methyl-2-oxazolyl,2-methoxy-4-oxazolyl, 2-hydroxy-4-oxazolyl, 3-isoxazolyl, 4-isoxazolyl,3-methyl-4-isoxazolyl, 4-methyl-3-isoxazolyl, 5-methyl-3-isoxazolyl,2-thiazolyl, 4-thiazolyl, 5othiazolyl, 4-methyl-2-thiazolyl,5-methyl-2-thiazolyl, 2-methyl-4-thiazolyl, 5-methyl-4-thiazolyl,2-methyl-5-thiazolyl, 4-methyl-5-thiazolyl, 2-methoxy-4-thiazolyl,2-methoxy-5-thiazolyl, 2-hydroxy-4-thiazolyl, 2-hydroxy-5-thiazolyl,5-chloro-2-thiazolyl, 2-chloro-4-thiazolyl, 5-chloro-4-thiazolyl,2-chloro-5-thiazolyl, 4-chloro-5-thiazolyl, 2-amino-4-thiazolyl,5-amino-4-thiazolyl, 2-amino-5-thiazolyl, 2-acetamido-4-thiazolyl,5-acetamido-4-thiazolyl, 2-acetamido-5-thiazolyl, 3-isothiazolyl,4-isothiazolyl, 3-pyrazolyl, 4-pyrazolyl, 1-methyl-4-pyrazolyl,3-methyl-4-pyrazolyl, 1-methyl-3-pyrazolyl, 4-methyl-3-pyrazolyl,5-methyl-3-pyrazolyl, 1-methyl-5-pyrazolyl, 1-ethyl-4-pyrazolyl,1-ethyl-3-pyrazolyl, 5-ethyl-3-pyrazolyl, 1-propyl-4-pyrazolyl,1-propyl-3-pyrazolyl, 5-propyl-3-pyrazolyl, 1-butyl-4-pyrazolyl,4-methoxy-3-pyrazolyl, 4-chloro-3-pyrazolyl, 3-chloro-4-pyrazolyl,4-bromo-3-pyrazolyl, 4-amino-3-pyrazolyl, 5-amino-3-pyrazolyl,3-amino-4-pyrazolyl, 3-acetamido-4-pyrazolyl,3-propionylamino-4-pyrazolyl, 4-acetamido-3-pyrazolyl,5oacetamido-3-pyrazolyl, 5-phenyl-3-pyrazolyl,1-(2-hydroxyethyl)-3-pyrazolyl, 1-(3-hydroxypropyl)-3-pyrazolyl,1-(2-hydroxyethyl)-4-pyrazolyl, 1-(3-hydroxypropyl)-4-pyrazolyl,1-(2-hydroxyethyl)-5-pyrazolyl, 1-(3-hydroxypropyl)-5-pyrazolyl,1,3-dimethyl-4-pyrazolyl, 1,5-dimethyl -4-pyrazolyl,3,5-dimethyl-4-pyrazolyl, 1,4-dimethyl -3-pyrazolyl,1,5-dimethyl-3-pyrazolyl, 4,5-dimethyl -3-pyrazolyl,1,3-dimethyl-5-pyrazolyl, 1,4-dimethyl -5-pyrazolyl,1-methyl-3-amino-4-pyrazolyl, 1-methyl-5-amino-4-pyrazolyl,5-methyl-3-amino-4-pyrazolyl, 1-methyl-3-acetamido-4-pyrazolyl,1-methyl-5-acetamido-4-pyrazolyl, 3-methyl-5-acetamido-4-pyrazolyl,1-methyl-5-amino-3-pyrazolyl, 5-methyl-4-amino-3-pyrazolyl,4-methyl-5-amino-3-pyrazolyl, 2-imidazolyl, 4-imidazolyl,1-methyl-2-imidazolyl, 5-methyl-2-imidazolyl, 1-methyl-4-imidazolyl,2-methyl-4-imidazolyl, 5-methyl-4-imidazolyl, 1-ethyl-2-imidazolyl,4-ethyl-2-imidazolyl, 1-(2-hydroxyethyl)-2-imidazolyl,1-(3-hydroxypropyl)-2-imidazolyl, 4-amino-2-imidazolyl,2-amino-4-imidazolyl, 5-amino-4-imidazolyl, 4-chloro-2-imidazoly,2-chloro-4-imidazolyl, 5-chloro-4-imidazolyl, 1,2,3-oxadiazol-4-yl,1,2,3-oxadiazol-5-yl, 5-methyl-1,2,3-oxadiazol-4-yl,4-methyl-1,2,3-oxadiazol-5-yl, 1,2,4-oxadiazol-3-yl,1,2,4-oxadiazol-5-yl, 1,2,5-oxadiazol-3-yl,4-methyl-1,2,5-oxadiazol-3-yl, 4-phenyl-1,2,5-oxadiazol-3-yl,1,3,4-oxadiazol-2-yl, 5-methyl-1,3,4-oxadiazol-2-yl,5-ethyl-1,3,4-oxadiazol-2-yl, 5-phenyl-1,3,4-oxadiazol-2-yl,5-chloro-1,3,4-oxadiazol-2-yl, 5-amino-1,3,4-oxadiazol-2-yl,5-acetamido-1,3,4-oxadiazol-2-yl, 1,2,3-thiadiazol-4-yl,1,2,3-thiadiazol-5-yl, 5-methyl-1,2,3-thiadiazol-4-yl,5-phenyl-1,2,3-thiadiazol-4-yl, 4-methyl-1,2,3-thiadiazol-5-yl,1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl,4-methyl-1,2,5-thiadiazol-3-yl, 1,3,4-thiadiazol-2-yl,5-methyl-1,3,4-thiadiazol-2-yl, 5-ethyl-1,3,4-thiadiazol-2-yl,5-phenyl-1,3,4-thiadiazol-2-yl, 5-chloro-1,3,4-thiadiazol-2-yl,5-amino-1,3,4-thiadiazol-2-yl, 5-acetamido-1,3,4-thiadiazol-2-yl,1,2,3-triazol-4-yl, 1-methyl-1,2,3-triazol-4-yl,5-methyl-1,2,3-triazol-4-yl, 1,5-dimethyl-1,2,3-triazol-4-yl,1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, 1-methyl-1,2,4-triazol-3-yl,1-methyl-1,2,4-triazol-5-yl, 5-methyl-1,2,4-triazol-3-yl,5-ethyl-1,2,4-triazol-3-yl, 5-phenyl-1,2,4-triazol-3-yl,1-(2-hydroxyethyl)-1,2,4-triazol-3-yl,1-(3-hydroxypropyl)-1,2,4-triazol-3-yl,1-(2-hydroxyethyl)-1,2,4-triazol-5-yl,1-(3-hydroxypropyl)-1,2,4-triazol-5-yl, 5-chloro-1,2,4-triazol-3-yl,5-amino-1,2,4-triazol-3-yl, 5-acetamido-1,2,4-triazol-3-yl,1,3-dimethyl-1,2,4-triazol-5-yl, 1,5-dimethyl-1,2,4-triazol-3-yl,tetrazol-5-yl, 1-methyltetrazol-5-yl, 2-methyltetrazol-5-yl,1-ethyltetrazol-5-yl, 2-ethyltetrazol-5-yl, 1-phenyltetrazol-5-yl,2-phenyltetrazol-5-yl, 1- (2-hydroxyethyl)tetrazol-5-yl,2-(2-hydroxyethyl) tetrazol -5 -yl, 1-(2-hydroxypropyl) tetrazol-5 -yl,2- ( 2 - hydroxypropyl ) tet razol - 5 - yl, 1 - ( 3 - hydroxypropyl)-tetrazol-5 -yl, 2- (3 -hydroxypropyl ) tetrazol - 5 -yl, 2-pyridyl,3-pyridyl, 4-pyridyl, 3-methyl-2-pyridyl, 4-methyl-2-pyridyl,5-methyl-2-pyridyl, 6-methyl-2-pyridyl, 2-methyl-4-pyridyl,3-methyl-4-pyridyl, 3-chloro-2-pyridyl, 4-chloro-2-pyridyl,5-chloro-2-pyridyl, 6-chloro-2-pyridyl, 2-chloro-4-pyridyl,3-chloro-4-pyridyl, 3-amino-2-pyridyl, 4-amino-2-pyridyl,5-amino-2-pyridyl, 6-amino-2-pyridyl, 2-amino4-pyridyl,3-amino-4-pyridyl, 3-hydroxy-2-pyridyl, 4-hydroxy-2-pyridyl,5-hydroxy-2-pyridyl, 6-hydroxy2-pyridyl, 2-hydroxy-4-pyridyl,3-hydroxy-4-pyridyl, 3-phenyl-2-pyridyl, 4-phenyl-2-pyridyl,5-phenyl-2pyridyl, 6-phenyl-2-pyridyl, 2-phenyl-4-pyridyl,3-phenyl-4-pyridyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl,4-methyl-2-pyrimidinyl, 5-methyl-2pyrimidinyl, 2-methyl-4-pyrimidinyl, 5-methyl-4-pyrimidinyl, 6-methyl-4-pyrimidinyl, 4 -phenyl-2-pyrimidinyl,5-phenyl-2-pyrimidinyl, 2 -phenyl-4-pyrimidinyl, 5-phenyl-4-pyrimidinyl,6 -phenyl-4-pyrimidinyl, 4-chloro-2-pyrimidinyl, 5-chloro-2-pyrimidinyl, 2-chloro-4-pyrimidinyl, 5 -chloro-4-pyrimidinyl,6-chloro-4-pyrimidinyl, 4-amino-2-pyrimidinyl, 5-amino-2-pyrimidinyt,2-amino-4-pyrimidinyl, 5-amino-4-pyrimidinyl, 6-amino-4-pyrimidinyl,4-acetamido-2-pyrimidinyl, 5-acetamido-2-pyrimidinyl,2-acetamido-4-pyrimidinyl, 5-acetamido-4-pyrimidinyl,6-acetamido-4-pyrimidinyl, 4,5-dimethyl-2-pyrimidinyl,4,6-dimethyl-2-pyrimidinyl, 2,5-dimethyl-4-pyrimidinyl,2,6-dimethyl-4-pyrimidinyl, 4-amino-5-hydroxy-2-pyrimidinyl,4-amino-6-hydroxy-2-pyrimidinyl, 2-amino-5-hydroxy-4-pyrimidinyl,2-amino-6-hydroxypyrimidinyl, 5-amino-2-hydroxy-4-pyrimidinyl,6-amino-2-hydroxy-4-pyrimidinyl, 4,5-diamino-2-pyrimidinyl,4,6-diamino-2-pyrimidinyl, 2,5-diamino-4-pyrimidinyl,2,6-diamino-4-pyrimidinyl , 3-pyridazinyl, 4-pyridazinyl,4-methyl-3-pyridazinyl, 5 -methyl-3-pyridazinyl, 6-methyl-3-pyridazinyl,3 -methyl-4-pyridazinyl, 5-methyl-4-pyridazinyl, 6-methyl-4-pyridazinyl, 4-chloro-3-pyridazinyl, 5 -chloro-3-pyridazinyl,6-chloro-3-pyridazinyl, 3 -chloro-4-pyridazinyl, 5-chloro-4-pyridazinyl,6 -chloro-4-pyridazinyl, 4-hydroxy-3-pyridazinyl,5-hydroxy-3-pyridazinyl, 6- hydroxy-3-pyridazinyl,3-hydroxy-4-pyridazinyl, 5- hydroxy-4-pyridazinyl,6-hydroxy-4-pyridazinyl, 4- amino-3-pyridazinyl, 5-amino-3-pyridazinyl,6-amino-3-pyridazinyl, 3-amino-4-pyridazinyl, 5-amino-4-pyridazinyl,6-amino-4-pyridazinyl, 2-pyrazinyl, 3-methyl-2-pyrazinyl,5-methyl-2-pyrazinyl, 6-methyl-2-pyrazinyl, 3-amino-2-pyrazinyl,5-amino-2-pyrazinyl, 6-amino-2-pyrazinyl, 3-hydroxy-2-pyrazinyl,5-hydroxy-2-pyrazinyl, 6-hydroxy-2-pyrazinyl, 3,5-dihydroxy-2-pyrazinyl,3,6-dihydroxy-2-pyrazinyl, 1,2,3-triazin-4-yl, 1,2,3-triazin-5-yl,5-methyl-1,2,3-triazin-4-yl, 6-methyl-1,2,3-triazin-4-yl,4-methyl-1,2,3-triazin-5-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl,1,2,4-triazin-6-yl, 5-methyl-1,2,4-triazin-3-yl,6-methyl-1,2,4-triazin-3-yl, 3-methyl-1,2,4-triazin-5-yl,6-methyl-1,2,4-triazin-5-yl, 3-methyl-1,2,4-triazin-6-yl,5-methyl-1,2,4-triazin-6-yl, 1,3,5-triazin-2-yl and4-methyl-1,3,5-triazin-2-yl groups.

Examples of more preferred such groups include: the 2-imidazolyl,4-imidazolyl, 1-methyl-2-imidazolyl, 5-methyl-2-imidazolyl,1-methyl-4-imidazolyl, 2-methyl-4-imidazolyl, 5-methyl-4-imidazolyl,4-chloro-2-imidazolyl, 2-chloro-4-imidazolyl, 5-chloro-4-imidazolyl,1,3,4-oxadiazol-2-yl, 5-methyl-1,3,4-oxadiazol-2-yl,5-ethyl-1,3,4-oxadiazol-2-yl, 5-chloro-1,3,4-oxadiazol-2-yl,5-amino-1,3,4-oxadiazol-2-yl, 5-acetamido-1,3,4-oxadiazol-2-yl,1,3,4-thiadiazol-2-yl, 5-methyl-1,3,4-thiadiazol-2-yl,5-ethyl-1,3,4-thiadiazol-2-yl, 5-chloro-1,3,4-thiadiazol-2-yl,5-amino-1,3,4-thiadiazol-2-yl, 5-acetamido-1,3,4-thiadiazol-2-yl,1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, 1-methyl-1,2,4-triazol-3-yl,1-methyl-1,2,4-triazol-5-yl, 5-methyl-1,2,4-triazol-3-yl,5-ethyl-1,2,4-triazol-3-yl, 5-phenyl-1,2,4-triazol-3-yl,5-chloro-1,2,4-triazol-3-yl, 5-amino-1,2,4-triazol-3-yl,5-acetamido-1,2,4triazol-3-yl, tetrazol-5-yl, 1-methyltetrazol-5-yl,1-ethyltetrazol-5-yl, 2-pyridyl, 3-pyridyl, 4-pyridyl,3-methyl-2-pyridyl, 4-methyl-2-pyridyl, 5-methyl-2-pyridyl,6-methyl-2-pyridyl, 2-methyl-4-pyridyl, 3-methyl-4-pyridyl,3-chloro-2-pyridyl, 4-chloro-2-pyridyl, 5-chloro-2-pyridyl,6-chloro-2-pyridyl, 2-chloro-4-pyridyl, 3-chloro-4-pyridyl,3-amino-2-pyridyl, 4-amino-2-pyridyl, 5-amino-2-pyridyl,6-amino-2-pyridyl, 2-amino-4-pyridyl, 3-amino-4-pyridyl,3-hydroxy-2-pyridyl, 4-hydroxy-2-pyridyl, 5-hydroxy-2-pyridyl,6-hydroxy-2-pyridyl, 2-hydroxy-4-pyridyl, 3-hydroxy-4-pyridyl,2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 4-methyl-2-pyrimidinyl,5-methyl-2-pyrimidinyl, 2-methyl-4-pyrimidinyl, 5-methyl-4-pyrimidinyl,6-methyl-4-pyrimidinyl, 4-chloro-2-pyrimidinyl, 5-chloro-2-pyrimidinyl,2-chloro-4-pyrimidinyl, 5-chloro-4-pyrimidinyl, 6-chloro-4-pyrimidinyl,4-amino-2-pyrimidinyl, 5-amino-2-pyrimidinyl, 2-amino-4-pyrimidinyl,5-amino-4-pyrimidinyl, 6-amino-4-pyrimidinyl, 4-acetamido-2-pyrimidinyl,5-acetamido-2-pyrimidinyl, 2-acetamido-4-pyrimidinyl,5-acetamido-4-pyrimidinyl, 6-acetamido-4-pyrimidinyl,4-amino-5-hydroxy-2-pyrimidinyl, 4-amino-6-hydroxy-2-pyrimidinyl,2-amino-5-hydroxy-4-pyrimidinyl, 2-amino-6-hydroxy-4-pyrimidinyl,5-amino-2-hydroxy-4-pyrimidinyl, 6-amino-2-hydroxy-4-pyrimidinyl,4,5-diamino-2-pyrimidinyl, 4,6-diamino-2-pyrimidinyl,2,5-diamino-4-pyrimidinyl and 2,6-diamino-4-pyrimidinyl groups.

Examples of still more preferred such groups include: the 2-imidazolyl,4-imidazolyl, 1,3,4-oxadiazol-2-yl, 5-methyl-1,3,4-oxadiazol-2-yl,1,3,4-thiadiazol-2-yl, 5-methyl-1,3,4-thiadiazol-2-yl,1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, 1-methyl-1,2,4-triazol-3-yl,1-methyl-1,2,4-triazol-5-yl, 5-methyl-1,2,4-triazol-3-yl, tetrazol-5-yl,1-methyltetrazol-5-yl, 2-pyridyl, 3-pyridyl, 4-pyridyl,3-methyl-2-pyridyl, 4-methyl-2-pyridyl, 5-methyl-2-pyridyl,6-methyl-2-pyridyl, 2-methyl-4-pyridyl, 3-methyl-4-pyridyl,3-amino-2-pyridyl, 4-amino-2-pyridyl, 5-amino-2-pyridyl,6-amino-2-pyridyl, 2-amino-4-pyridyl, 3-amino-4-pyridyl,3-hydroxy-2-pyridyl, 4-hydroxy-2-pyridyl, 5-hydroxy-2-pyridyl,6-hydroxy-2-pyridyl, 2-hydroxy-4opyridyl, 3-hydroxy-4-pyridyl,2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 4-methyl-2-pyrimidinyl,5-methyl-2-pyrimidinyl, 2-methyl-4-pyrimidinyl, 5-methyl-4-pyrimidinyl,6-methyl-4-pyrimidinyl, 4-amin-2-pyrimidinyl, 5-amino-2-pyrimidinyl,2-amino-4-pyrimidinyl, 5-amino-4-pyrimidinyl, 6-amino-4-pyrimidinyl,4-amino-5-hydroxy-2-pyrimidinyl, 4-amino-6-hydroxy-2-pyrimidinyl,2-amino-5-hydroxy-4-pyrimidinyl 2-amino-6-hydroxy-4opyrimidinyl,5-amino-2ohydroxy-4-pyrimidinyl and 6-amino-2-hydroxy-4-pyrimidinylgroups.

Examples of the most preferred such groups include: the1,3,4-oxadiazol-2-yl, 5-methyl-1,3,4-oxadiazol-2-yl,1,3,4-thiadiazol-2-yl, 1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl,1-methyl-1,2,4-triazol-3-yl, 1-methyl-1,2,4-triazol-5-yl,5-methyl-1,2,4-triazol-3-yl, 2-pyridyl, 3-pyridyl, 4-pyridyl,2-pyrimidinyl, 4-pyrimidinyl, 4-methyl-2-pyrimidinyl,5-methyl-2-pyrimidinyl, 2-methyl-4-pyrimidinyl, 5-methyl-4-pyrimidinyland 6-methyl-4-pyrimidinyl groups.

The compounds of the present invention can form salts. Where thecompound contains a carboxy group, it can form a salt with a cation.Examples of such salts include: salts with an alkali metal, such assodium, potassium or lithium; salts with an alkaline earth metal, suchas barium or calcium; salts with another metal, such as magnesium oraluminum; ammonium salts; organic base salts, such as a salt withtriethylamine, diisopropylamine, cyclohexylamine or dicyclohexylamine;and salts with a basic amino acid, such as lysine or arginine. Also,since the compounds of the present invention necessarily contain basicgroups in their molecules, they can form acid addition salts. Examplesof such acid addition salts include: salts with mineral acids,especially hydrohalic acids (such as hydrofluoric acid, hydrobromicacid, hydroiodic acid or hydrochloric acid), nitric acid, perchloricacid, carbonic acid, sulfuric acid or phosphoric acid; salts with loweralkylsulfonic acids, such as methanesulfonic acid,trifluoromethanesulfonic acid or ethanesulfonic acid; salts witharylsulfonic acids, such as benzenesulfonic acid or p-toluenesulfonicacid; salts with organic carboxylic acids, such as acetic acid, fumaricacid, tartaric acid, oxalic acid, maleic acid, malic acid, succinicacid, benzoic acid, mandelic acid, ascorbic acid, lactic acid, gluconicacid, citric acid or 2-(4-hydroxybenzoyl)benzoic acid; and salts withamino acids, such as glutamic acid or aspartic acid.

The compounds of the present invention may contain several asymmetriccarbon atoms in their molecules, and can thus form optical isomers.Although these are all represented herein by a single molecular formula,the present invention includes both the individual, isolated isomers andmixtures, including racemates thereof. Where stereospecific synthesistechniques are employed or optically active compounds are employed asstarting materials, individual isomers may be prepared directly; on theother hand, if a mixture of isomers is prepared, the individual isomersmay be obtained by conventional resolution techniques.

Of the compounds of the present invention, we prefer those wherein R¹represents a cyclic amino group having from 3 to 7 ring atoms, of which1 is a nitrogen atom and the remainder are carbon atoms, or saiddialkylamino group, more preferably those wherein R¹ represents a cyclicamino group having 5 or 6 ring atoms, of which 1 is a nitrogen atom andthe remainder are carbon atoms, or said dialkylamino group, especiallythose wherein R¹ represents a 1-pyrrolidinyl, piperidino, dimethylaminoor diethylamino group.

Another preferred class of compounds of the present invention are thosewherein R² represents a group of formula --NHCHR³ R⁴ wherein R³ and R⁴are independently selected from the group consisting of:

alkyl groups having from 1 to 4 carbon atoms,

phenyl groups which are unsubstituted or have at least one substituentselected from the group consisting of substituents ζ, defined above, and

benzyl and phenethyl groups; or

R³ and R⁴ together with the carbon atom to which they are attached,represent a cycloalkyl group having from 3 to 6 ring carbon atoms,

An alternative preferred class of compounds of the present invention arethose wherein R² represents an aromatic heterocyclic group having 5 ringatoms, of which 1 is a hetero-atom selected from the group consisting ofnitrogen, oxygen and sulfur hetero-atoms, there are 0, 1 or 2 additionalnitrogen hetero-atoms, and the remaining ring atoms are carbon atoms,said group being unsubstituted or having at least one substituentselected, in the case of substituents on carbon atoms, from the groupconsisting of substituents α and, in the case of substituents onnitrogen atoms, from the group consisting of substituents β, as definedabove, and particularly those wherein said aromatic heterocyclic groupis selected from the group consisting of furyl, thienyl, pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl,oxadiazolyl and thiadiazolyl groups, which are unsubstituted or aresubstituted as defined above.

A further alternative preferred class of compounds of the presentinvention are those wherein R² represents a group of formula--B--S(O)_(m) --R⁵, wherein:

B represents an alkylene or alkylidene group having from 1 to 3 carbonatoms;

m is 0, 1 or 2; and

R⁵ represents: a substituted alkyl group which has from 2 to 4 carbonatoms and which is substituted at its 2-position by at least onesubstituent selected from the group consisting of substituents γ; or anaromatic heterocyclic group which has 5 or 6 ring atoms of which 1 is ahetero-atom selected from the group consisting of nitrogen, oxygen andsulfur hetero-atoms, there are 0, 1, 2 or 3 additional nitrogenhetero-atoms, and the remaining ring atoms are carbon atoms, said groupbeing unsubstituted or having at least one substituent selected, in thecase of substituents on carbon atoms, from the group consisting ofsubstituents α and, in the case of substituents on nitrogen atoms, fromthe group consisting of substituents ε, as defined above.

We also especially prefer those compounds of the present inventionwherein A represents a group of formula --CH═CH-- or --(CH₂)_(n) --,where n is 1 or 2.

A more preferred class of compounds of the present invention are thosewherein:

R¹ represents a 1-pyrrolidinyl, piperidino, dimethylamino ordiethylamino group;

R² represents

a group of formula --NHCHR³ R⁴ wherein

R³ and R⁴ are independently selected from the group consisting of alkylgroups having from 1 to 4 carbon atoms, benzyl groups, phenethyl groupsand phenyl groups which are unsubstituted or which are substituted by atleast one substituent selected from the group consisting of methyl,methoxy, fluorine atoms and chlorine atoms, or

R³ and R⁴ together with the carbon atom to which they are attached,represent a cycloalkyl group having from 3 to 6 ring carbon atoms,

a furyl, thienyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolyl,imidazolyl or thiadiazolyl group, which is unsubstituted or issubstituted by at least one substituent selected, in the case ofsubstituents on carbon atoms, from the group consisting of substituentsα¹ and, in the case of substituents on nitrogen atoms, from the groupconsisting of methyl and ethyl groups,

or a group of formula --B--S(O)_(m) --R⁵, wherein

R⁵ represents: a substituted ethyl or propyl group which is substitutedat its 2-position by at least one substituent selected from the groupconsisting of substituents γ¹ ; or an imidazolyl, 1,2,4-triazolyl,1,3,4-oxadiazolyl, 1,3,4-thiadiazolyl, tetrazolyl, pyridyl orpyrimidinyl group which is unsubstituted or has at least one substituentselected, in the case of substituents on carbon atoms, from the groupconsisting of substituents α¹ and, in the case of substituents onnitrogen atoms, from the group consisting of substituents ε¹,

B represents an alkylene or alkylidene group having from 1 to 3 carbonatoms,

and m is 0, 1 or 2;

A represents a group of formula --CH═CH-- or --(CH₂)_(n) --, where n is1 or 2;

said substituents α¹ are selected from the group consisting of: methylgroups, ethyl groups, methoxy groups, ethoxy groups, hydroxy groups,chlorine atoms, amino groups; methylamino groups, ethylamino groups,dimethylamino groups, diethylamino groups, alkanoylamino groups havingfrom 1 to 3 carbon atoms, phenyl groups, and substituted phenyl groupsin which the substituent is selected from the group consisting of methylgroups, methoxy groups, chlorine atoms and fluorine atoms;

said substituents γ¹ are selected from the group consisting of: hydroxygroups; alkanoyloxy groups having from 1 to 5 carbon atoms; substitutedalkanoyloxy groups which have 3 or 4 carbon atoms and which aresubstituted by at least one substituent selected from the groupconsisting of carboxy, methoxycarbonyl and ethoxycarbonyl groups;phenylacetoxy groups; benzoyloxy groups; and cycloalkylcarbonyloxygroups in which the cycloalkyl part has from 3 to 6 ring carbon atoms;

said substituents ε¹ are selected from the group consisting of: methylgroups, ethyl groups, and hydroxyalkyl groups having from 2 to 4 carbonatoms.

Still more preferred compounds of the present invention are thosecompounds of formula (I) and salts thereof, wherein:

R¹ represents a 1-pyrrolidinyl or piperidino group;

R² represents

a group of formula --NHCHR³ R⁴ wherein

R³ and R⁴ are independently selected from the group consisting ofmethyl, ethyl, phenyl and benzyl groups, or

R³ and R⁴, together with the carbon atom to which they are attached,represent a cycloalkyl group having from 3 to 5 ring carbon atoms,

a furyl, thienyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolylor 1,2,3-thiadiazolyl group, which is unsubstituted or is substituted byat least one substituent selected, in the case of substituents on carbonatoms, from the group consisting of substituents α² and, in the case ofsubstituents on nitrogen atoms, from the group consisting of methyl andethyl groups,

or a group of formula --B--S(O)_(m) --R⁵, wherein

R⁵ represents: a substituted ethyl or propyl group which is substitutedat its 2-position by at least one substituent selected from the groupconsisting of substituents γ² ; or a 1,2,4-triazolyl, 1,3,4-oxadiazolylor pyrimidinyl group which is unsubstituted or has at least onesubstituent selected, in the case of substituents on carbon atoms, fromthe group consisting of substituents α³ and, in the case of substituentson nitrogen atoms, from the group consisting of methyl and ethyl groups,

B represents an alkylene or alkylidene group having from 1 to 3 carbonatoms,

and m is 0 or 1;

A represents a group of formula --CH═CH-- or --(CH₂)₂ --;

said substituents α² are selected from the group consisting of: methylgroups, ethyl groups, methoxy groups, ethoxy groups, hydroxy groups,chlorine atoms, amino groups, acetamido groups and phenyl groups;

said substituents α³ are selected from the group consisting of: methylgroups, ethyl groups, methoxy groups, ethoxy groups, hydroxy groups,chlorine atoms, amino groups, and acetamido groups;

said substituents γ² are selected from the group consisting of: hydroxygroups; acetoxy groups; propionyloxy groups; substituted alkanoyloxygroups which have 3 or 4 carbon atoms and which are substituted by atleast one substituent selected from the group consisting of carboxy,methoxycarbonyl and ethoxycarbonyl groups; phenylacetoxy groups;benzoyloxy groups; and cycloalkylcarbonyloxy groups in which thecycloalkyl part has from 3 to 6 ring carbon atoms.

Yet more preferred compounds of the present invention are thosecompounds of formula (I) and salts thereof, wherein:

R¹ represents a piperidino group;

R² represents

a group of formula --NHCHR³ R⁴ wherein

R³ and R⁴ are independently selected from the group consisting ofmethyl, ethyl, phenyl and benzyl groups, or

R³ and R⁴ together with the carbon atom to which they are attached,represent a cycloalkyl group having 3 or 4 ring carbon atoms,

a thienyl, pyrrolyl, thiazolyl, pyrazolyl or 1,2,3-thiadiazolyl group,which is unsubstituted or is substituted by at least one substituentselected, in the case of substituents on carbon atoms, from the groupconsisting of substituents α⁴ and, in the case of substituents onnitrogen atoms, from methyl groups,

or a group of formula --B--S(O)_(m) --R⁵, wherein

B represents a methylene group and R⁵ represents: a substituted ethyl orpropyl group which is substituted at its 2-position by at least onesubstituent selected from the group consisting of substituents γ³ ; or

B represents a trimethylene group and R⁵ represents: a 1,2,4-triazolyl,1,3,4-oxadiazolyl or pyrimidinyl group which is unsubstituted or has atleast one substituent selected, in the case of substituents on carbonatoms, from the group consisting of methyl, hydroxy and amino groups,and, in the case of substituents on nitrogen atoms, from methyl groups,

and m is 0;

A represents a group of formula --CH=CH--;

said substituents α⁴ are selected from the group consisting of:methyl.groups, methoxy groups, hydroxy groups, chlorine atoms and aminogroups; said substituents γ³ are selected from the group consisting of:hydroxy groups; acetoxy groups; propionyloxy groups; substitutedpropionoyloxy groups which are substituted by at least one substituentselected from the group consisting of carboxy, methoxycarbonyl andethoxycarbonyl groups; benzoyloxy groups; and cycloalkylcarbonyloxygroups in which the cycloalkyl part has 5 or 6 ring carbon atoms.

The most preferred compounds of the present invention are thosecompounds of formula (I) and salts thereof, wherein:

R¹ represents a piperidino group;

R² represents:

a pyrazolyl group, which is unsubstituted or is substituted on a carbonatom by at least one amino substituent,

or a group of formula --B--S(O)_(m) --R⁵, wherein

B represents a methylene group and R⁵ represents: a substituted ethylgroup which is substituted at its 2-position by at least one substituentselected from the group consisting of substituents hydroxy, acetoxy,propionyloxy, benzoyloxy, cyclopentylcarbonyloxy andcyclohexylcarbonyloxy groups; or

B represents a trimethylene group and R⁵ represents: a 2-pyrimidinylgroup;

and m is 0;

A represents a group of formula --CH═CH--.

Examples of specific preferred compounds of the present invention arethose compounds of formula (I-1), in which the substituents are asdefined in Table 1, and those compounds of formula (I-1), in which thesubstituents are as defined in Tables 2 and 3. ##STR4##

In the Tables, the following abbreviations are used:

    ______________________________________                                        Ac                 acetyl                                                     Aze                azetidino                                                  Azi                aziridino                                                  Boz                benzoyl                                                    Bu                 butyl                                                      cBu                cyclobutyl                                                 iBu                isobutyl                                                   sBu                sec-butyl                                                  Byr                butyryl                                                    iByr               isobutyryl                                                 Bz                 benzyl                                                     Et                 ethyl                                                      Etc                ethoxycarbonyl                                             Fo                 formyl                                                     Fur                furyl                                                      Hp                 heptyl                                                     cHp                cycloheptyl                                                Hx                 hexyl                                                      cHx                cyclohexyl                                                 iHx                isohexyl                                                   Imidazo            imidazolyl                                                 Isoxazo            isoxazolyl                                                 Isothiazo          isothiazolyl                                               Me                 methyl                                                     Mec                methoxycarbonyl                                            Naph               naphthyl                                                   cOc                cyclooctyl                                                 Oxazo              oxazolyl                                                   Oxadiazo           oxadiazolyl                                                Ph                 phenyl                                                     Phc                phenoxycarbonyl                                            Pip                piperidino                                                 Piv                pivaloyl                                                   Pn                 pentyl                                                     cPn                cyclopentyl                                                iPn                isopentyl                                                  nPn                neopentyl                                                  Pr                 propyl                                                     cPr                cyclopropyl                                                iPr                isopropyl                                                  Prc                propoxycarbonyl                                            Prn                propionyl                                                  Pyl                pyrrolyl                                                   Pymz               pyrimidinyl                                                Pyr                1-pyrrolidinyl                                             Pyrazo             pyrazolyl                                                  Pyz                pyridyl                                                    Tetrazo            tetrazolyl                                                 Thi                thienyl                                                    Thiazo             thiazolyl                                                  Thiadiazo          thiadiazolyl                                               Triazo             triazolyl                                                  Val                valeryl                                                    iVal               isovaleryl.                                                ______________________________________                                    

                  TABLE 1                                                         ______________________________________                                        Cpd.                                                                          No.      R.sup.1  A         R.sup.2                                           ______________________________________                                        1-1      Pip      CH═CH 2-Fur                                             1-2      Pip      CH═CH 3-Fur                                             1-3      Pip      CH═CH 4-Me-2-Fur                                        1-4      Pip      CH═CH 5-Me-2-Fur                                        1-5      Pip      CH═CH 2-Me-3-Fur                                        1-6      Pip      CH═CH 5-Me-3-Fur                                        1-7      Pip      CH═CH 5-Cl-2-Fur                                        1-8      Pip      CH═CH 5-Cl-3-Fur                                        1-9      Pip      CH═CH 5-NH.sub.2 -2-Fur                                 1-10     Pip      CH═CH 5-AcNH-2-Fur                                      1-11     Pip      CH═CH 5-Ph-2-Fur                                        1-12     Pip      CH═CH 5-(4-MePh)-2-Fur                                  1-13     Pip      CH═CH 5-(4-ClPh)-2-Fur                                  1-14     Pip      CH═CH 3-Me-5-NH.sub.2 -2-Fur                            1-15     Pip      CH═CH 2,4-diMe-3-Fur                                    1-16     Pip      CH═CH 2-Thi                                             1-17     Pip      CH═CH 3-Thi                                             1-18     Pip      CH═CH 3-Me-2-Thi                                        1-19     Pip      CH═CH 5-Me-2-Thi                                        1-20     Pip      CH═CH 2-Me-3-Thi                                        1-21     Pip      CH═CH 4-Me-3-Thi                                        1-22     Pip      CH═CH 5-Me-3-Thi                                        1-23     Pip      CH═CH 4-MeO-2-Thi                                       1-24     Pip      CH═CH 4-MeO-3-Thi                                       1-25     Pip      CH═CH 4-HO-2-Thi                                        1-26     Pip      CH═CH 4-HO-3-Thi                                        1-27     Pip      CH═CH 5-Et-2-Thi                                        1-28     Pip      CH═CH 5-Cl-2-Thi                                        1-29     Pip      CH═CH 5-Cl-3-Thi                                        1-30     Pip      CH═CH 5-Br-3-Thi                                        1-31     Pip      CH═CH 3-NH.sub.2 -2-Thi                                 1-32     Pip      CH═CH 5-NH.sub.2 -2-Thi                                 1-33     Pip      CH═CH 2-NH.sub.2 -3-Thi                                 1-34     Pip      CH═CH 4-NH.sub.2 -3-Thi                                 1-35     Pip      CH═CH 3-AcNH-2-Thi                                      1-36     Pip      CH═CH 4-AcNH-3-Thi                                      1-37     Pip      CH═CH 5-Ph-2-Thi                                        1-38     Pip      CH═CH 4,5-diMe-2-Thi                                    1-39     Pip      CH═CH 3,5-diMe-2-Thi                                    1-40     Pip      CH═CH 2,5-diMe-3-Thi                                    1-41     Pip      CH═CH 4,5-diMe-3-Thi                                    1-42     Pip      CH═CH 4,5-diCl-2-Thi                                    1-43     Pip      CH═CH 2-NH.sub.2 -5-Ph-3-Thi                            1-44     Pip      CH═CH 4-NH.sub.2 -2,5-diMe-3-Thi                        1-45     Pip      CH═CH 2-Pyl                                             1-46     Pip      CH═CH 3-Pyl                                             1-47     Pip      CH═CH 1-Me-2-Pyl                                        1-48     Pip      CH═CH 3-Me-2-Pyl                                        1-49     Pip      CH═CH 4-Me-2-Pyl                                        1-50     Pip      CH═CH 2-Me-3-Pyl                                        1-51     Pip      CH═CH 5-Me-3-Pyl                                        1-52     Pip      CH═CH 3-NH.sub.2 -2-Pyl                                 1-53     Pip      CH═CH 4-NH.sub.2 -2-Pyl                                 1-54     Pip      CH═CH 3-AcNH-2-Pyl                                      1-55     Pip      CH═CH 5-Cl-2-Pyl                                        1-56     Pip      CH═CH 5-Cl-3-Pyl                                        1-57     Pip      CH═CH 4-Ph-2-Pyl                                        1-58     Pip      CH═CH 5-Ph-3-Pyl                                        1-59     Pip      CH═CH 1-Me-4-MeO-3-Pyl                                  1-60     Pip      CH═CH 1-Me-4-HO-3-Pyl                                   1-61     Pip      CH═CH 3,5-diMe-2-Pyl                                    1-62     Pip      CH═CH 4,5-diMe-2-Pyl                                    1-63     Pip      CH═CH 1,3-diMe-2-Pyl                                    1-64     Pip      CH═CH 5-NH.sub.2 -1-Me-2-Pyl                            1-65     Pip      CH═CH 4-NH.sub.2 -3,5-diMe-2-Pyl                        1-66     Pip      CH═CH 5-Br-1,4-diMe-3-Pyl                               1-67     Pip      CH═CH 4-Oxazo                                           1-68     Pip      CH═CH 5-Oxazo                                           1-69     Pip      CH═CH 2-Oxazo                                           1-70     Pip      CH═CH 2-Me-4-Oxazo                                      1-71     Pip      CH═CH 2-Ph-4-Oxazo                                      1-72     Pip      CH═CH 5-Ph-2-Oxazo                                      1-73     Pip      CH═CH 2-HO-4-Oxazo                                      1-74     Pip      CH═CH 2,5-diMe-4-Oxazo                                  1-75     Pip      CH═CH 4-Me-2-Ph-5-Oxazo                                 1-76     Pip      CH═CH 3-Isoxazo                                         1-77     Pip      CH═CH 4-Isoxazo                                         1-78     Pip      CH═CH 4-Me-3-Isoxazo                                    1-79     Pip      CH═CH 5-Me-3-Isoxazo                                    1-80     Pip      CH═CH 3-Me-4-Isoxazo                                    1-81     Pip      CH═CH 4-MeO-3-Isoxazo                                   1-82     Pip      CH═CH 4-HO-3-Isoxazo                                    1-83     Pip      CH═CH 3-HO-4-Isoxazo                                    1-84     Pip      CH═CH 3-HO-5-Isoxazo                                    1-85     Pip      CH═CH 4-NH.sub.2 -3-Isoxazo                             1-86     Pip      CH═CH 5-NH.sub.2 -4-Isoxazo                             1-87     Pip      CH═CH 5-Ph-3-Isoxazo                                    1-88     Pip      CH═CH 4-Ph-3-Isoxazo                                    1-89     Pip      CH═CH 4,5-diMe-3-Isoxazo                                1-90     Pip      CH═CH 4-HO-5-Me-3-Isoxazo                               1-91     Pip      CH═CH 2-Thiazo                                          1-92     Pip      CH═CH 4-Thiazo                                          1-93     Pip      CH═CH 5-Thiazo                                          1-94     Pip      CH═CH 4-Me-2-Thiazo                                     1-95     Pip      CH═CH 2-Me-4-Thiazo                                     1-96     Pip      CH═CH 2-Me-5-Thiazo                                     1-97     Pip      CH═CH 2-MeO-4-Thiazo                                    1-98     Pip      CH═CH 2-MeO-5-Thiazo                                    1-99     Pip      CH═CH 2-HO-4-Thiazo                                     1-100    Pip      CH═CH 2-HO-5-Thiazo                                     1-101    Pip      CH═CH 2-Cl-5-Thiazo                                     1-102    Pip      CH═CH 5-Cl-2-Thiazo                                     1-103    Pip      CH═CH 2-NH.sub.2 -4-Thiazo                              1-104    Pip      CH═CH 2-NH.sub.2 -5-Thiazo                              1-105    Pip      CH═CH 5-NH.sub.2 -4-Thiazo                              1-106    Pip      CH═CH 2-AcNH-4-Thiazo                                   1-107    Pip      CH═CH 5-AcNH-4-Thiazo                                   1-108    Pip      CH═CH 2-Ph-4-Thiazo                                     1-109    Pip      CH═CH 4,5-diMe-2-Thiazo                                 1-110    Pip      CH═CH 2-HO-5-Me-4-Thiazo                                1-111    Pip      CH═CH 5-NH.sub.2 -2-Me-4-Thiazo                         1-112    Pip      CH═CH 2-Cl-4-Me-5-Thiazo                                1-113    Pip      CH═CH 3-Isothiazo                                       1-114    Pip      CH═CH 4-Isothiazo                                       1-115    Pip      CH═CH 3-Pyrazo                                          1-116    Pip      CH═CH 4-Pyrazo                                          1-117    Pip      CH═CH 1-Me-3-Pyrazo                                     1-118    Pip      CH═CH 1-Et-3-Pyrazo                                     1-119    Pip      CH═CH 1-Pr-3-Pyrazo                                     1-120    Pip      CH═CH 1-Me-4-Pyrazo                                     1-121    Pip      CH═CH 1-Et-4-Pyrazo                                     1-122    Pip      CH═CH 1-Pr-4-Pyrazo                                     1-123    Pip      CH═CH 1-Bu-4-Pyrazo                                     1-124    Pip      CH═CH 4-Me-3-Pyrazo                                     1-125    Pip      CH═CH 5-Me-3-Pyrazo                                     1-126    Pip      CH═CH 5-Et-3-Pyrazo                                     1-127    Pip      CH═CH 5-Pr-3-Pyrazo                                     1-128    Pip      CH═CH 5-Me-4-Pyrazo                                     1-129    Pip      CH═CH 4-MeO-3-Pyrazo                                    1-130    Pip      CH═CH 4-PrO-3-Pyrazo                                    1-131    Pip      CH═CH 4-HO-3-Pyrazo                                     1-132    Pip      CH═CH 4-Cl-3-Pyrazo                                     1-133    Pip      CH═CH 4-Br-3-Pyrazo                                     1-134    Pip      CH═CH 3-Cl-4-Pyrazo                                     1-135    Pip      CH═CH 4-NH.sub.2 -3-Pyrazo                              1-136    Pip      CH═CH 5-NH.sub.2 -3-Pyrazo                              1-137    Pip      CH═CH 3-NH.sub.2 -4-Pyrazo                              1-138    Pip      CH═CH 4-AcNH-3-Pyrazo                                   1-139    Pip      CH═CH 5-AcNH-3-Pyrazo                                   1-140    Pip      CH═CH 3-AcNH-4-Pyrazo                                   1-141    Pip      CH═CH 3-EtCONH-4-Pyrazo                                 1-142    Pip      CH═CH 5-Ph-3-Pyrazo                                     1-143    Pip      CH═CH 1,5-diMe-3-Pyrazo                                 1-144    Pip      CH═CH 1,4-diMe-3-Pyrazo                                 1-145    Pip      CH═CH 4,5-diMe-3-Pyrazo                                 1-146    Pip      CH═CH 3-Me-4-Pyrazo                                     1-147    Pip      CH═CH 3,5-diMe-4-Pyrazo                                 1-148    Pip      CH═CH 1,5-diMe-4-Pyrazo                                 1-149    Pip      CH═CH 1,3-diMe-4-Pyrazo                                 1-150    Pip      CH═CH 1,3-diMe-5-Pyrazo                                 1-151    Pip      CH═CH 3-Cl-5-Me-4-Pyrazo                                1-152    Pip      CH═CH 3-Cl-1-Me-4-Pyrazo                                1-153    Pip      CH═CH 5-Cl-1-Me-4-Pyrazo                                1-154    Pip      CH═CH 4-Cl-1-Me-3-Pyrazo                                1-155    Pip      CH═CH 4-Cl-5-Me-3-Pyrazo                                1-156    Pip      CH═CH 4-Cl-1-Me-3-Pyrazo                                1-157    Pip      CH═CH 3-NH.sub.2 -5-Me-4-Pyrazo                         1-158    Pip      CH═CH 3-NH.sub.2 -1-Me-4-Pyrazo                         1-159    Pip      CH═CH 5-NH.sub.2 -1-Me-4-Pyrazo                         1-160    Pip      CH═CH 5-NH.sub.2 -4-Me-3-Pyrazo                         1-161    Pip      CH═CH 5-NH.sub.2 -1-Me-3-Pyrazo                         1-162    Pip      CH═CH 5-AcNH-1-Me-4-Pyrazo                              1-163    Pip      CH═CH 4-NH.sub.2 -5-Me-3-Pyrazo                         1-164    Pip      CH═CH 4-HO-5-Me-3-Pyrazo                                1-165    Pip      CH═CH 5-AcNH-3-Me-4-Pyrazo                              1-166    Pip      CH═CH 1,3,5-triMe-4-Pyrazo                              1-167    Pip      CH═CH 1,3,4-triMe-5-Pyrazo                              1-168    Pip      CH═CH 4-Cl-1,3-diMe-5-Pyrazo                            1-169    Pip      CH═CH 2-Imidazo                                         1-170    Pip      CH═CH 4-Imidazo                                         1-171    Pip      CH═CH 2-Me-4-Imidazo                                    1-172    Pip      CH═CH 1-Me-4-Imidazo                                    1-173    Pip      CH═CH 5-Me-4-Imidazo                                    1-174    Pip      CH═CH 5-Me-2-Imidazo                                    1-175    Pip      CH═CH 1-Me-2-Imidazo                                    1-176    Pip      CH═CH 1,2,3-Oxadiazo-5-yl                               1-177    Pip      CH═CH 1,3,4-Oxadiazo-2-yl                               1-178    Pip      CH═CH 1,2,3-Oxadiazo-4-yl                               1-179    Pip      CH═CH 1,2,4-Oxadiazo-5-yl                               1-180    Pip      CH═CH 1,2,4-Oxadiazo-3-yl                               1-181    Pip      CH═CH 1,2,5-Oxadiazo-3-yl                               1-182    Pip      CH═CH 5-Me-1,2,3-Oxadiazo-4-yl                          1-183    Pip      CH═CH 4-Me-1,2,5-Oxadiazo-3-yl                          1-184    Pip      CH═CH 4-Ph-1,2,5-Oxadiazo-3-yl                          1-185    Pip      CH═CH 1,2,3-Thiadiazo-4-yl                              1-186    Pip      CH═CH 1,2,3-Thiadiazo-5-yl                              1-187    Pip      CH═CH 1,3,4-Thiadiazo-2-yl                              1-188    Pip      CH═CH 1,2,4-Thiadiazo-3-yl                              1-189    Pip      CH═CH 1,2,4-Thiadiazo-5-yl                              1-190    Pip      CH═CH 1,2,5-Thiadiazo-3-yl                              1-191    Pip      CH═CH 4-Me-1,2,3-Thiadiazo-5-yl                         1-192    Pip      CH═CH 5-Me-1,2,3-Thiadiazo-4-yl                         1-193    Pip      CH═CH 4-Me-1,2,5-Thiadiazo-3-yl                         1-194    Pip      CH═CH 5-Ph-1,2,3-Thiadiazo-4-yl                         1-195    Pyr      CH═CH 2-Fur                                             1-196    Pyr      CH═CH 3-Fur                                             1-197    Pyr      CH═CH 4-Me-2-Fur                                        1-198    Pyr      CH═CH 2-Me-3-Fur                                        1-199    Pyr      CH═CH 2,4-diMe-3-Fur                                    1-200    Pyr      CH═CH 2-Thi                                             1-201    Pyr      CH═CH 3-Thi                                             1-202    Pyr      CH═CH 3-Me-2-Thi                                        1-203    Pyr      CH═CH 2-Me-3-Thi                                        1-204    Pyr      CH═CH 4-Me-3-Thi                                        1-205    Pyr      CH═CH 4-MeO-3-Thi                                       1-206    Pyr      CH═CH 4-HO-2-Thi                                        1-207    Pyr      CH═CH 5-Cl-3-Thi                                        1-208    Pyr      CH═CH 3-NH.sub.2 -2-Thi                                 1-209    Pyr      CH═CH 2-NH.sub.2 -3-Thi                                 1-210    Pyr      CH═CH 3-AcNH-2-Thi                                      1-211    Pyr      CH═CH 5-Ph-2-Thi                                        1-212    Pyr      CH═CH 4,5-diMe-2-Thi                                    1-213    Pyr      CH═CH 2,5-diMe-3-Thi                                    1-214    Pyr      CH═CH 4,5-diCl-2-Thi                                    1-215    Pyr      CH═CH 4-NH.sub.2 -2,5-diMe-3-Thi                        1-216    Pyr      CH═CH 2-Pyl                                             1-217    Pyr      CH═CH 3-Pyl                                             1-218    Pyr      CH═CH 1-Me-2-Pyl                                        1-219    Pyr      CH═CH 3-Me-2-Pyl                                        1-220    Pyr      CH═CH 4-Me-2-Pyl                                        1-221    Pyr      CH═CH 2-Me-3-Pyl                                        1-222    Pyr      CH═CH 1-Me-4-MeO-3-Pyl                                  1-223    Pyr      CH═CH 3,5-diMe-2-Pyl                                    1-224    Pyr      CH═CH 1,3-diMe-2-Pyl                                    1-225    Pyr      CH═CH 4-Oxazo                                           1-226    Pyr      CH═CH 5-Oxazo                                           1-227    Pyr      CH═CH 2-Oxazo                                           1-228    Pyr      CH═CH 2-Me-4-Oxazo                                      1-229    Pyr      CH═CH 5-Ph-2-Oxazo                                      1-230    Pyr      CH═CH 2,5-diMe-4-Oxazo                                  1-231    Pyr      CH═CH 3-Isoxazo                                         1-232    Pyr      CH═CH 4-Isoxazo                                         1-233    Pyr      CH═CH 5-Me-3-Isoxazo                                    1-234    Pyr      CH═CH 3-Me-4-Isoxazo                                    1-235    Pyr      CH═CH 4-MeO-3-Isoxazo                                   1-236    Pyr      CH═CH 4-HO-3-Isoxazo                                    1-237    Pyr      CH═CH 3-HO-5-Isoxazo                                    1-238    Pyr      CH═CH 5-HO-4-Isoxazo                                    1-239    Pyr      CH═CH 4-NH.sub.2 -3-Isoxazo                             1-240    Pyr      CH═CH 5-Ph-3-Isoxazo                                    1-241    Pyr      CH═CH 4,5-diMe-3-Isoxazo                                1-242    Pyr      CH═CH 4-HO-5-Me-3-Isoxazo                               1-243    Pyr      CH═CH 2-Thiazo                                          1-244    Pyr      CH═CH 4-Thiazo                                          1-245    Pyr      CH═CH 5-Thiazo                                          1-246    Pyr      CH═CH 4-Me-2-Thiazo                                     1-247    Pyr      CH═CH 2-Me-5-Thiazo                                     1-248    Pyr      CH═CH 2-MeO-4-Thiazo                                    1-249    Pyr      CH═CH 2-MeO-5-Thiazo                                    1-250    Pyr      CH═CH 2-HO-5-Thiazo                                     1-251    Pyr      CH═CH 5-Cl-2-Thiazo                                     1-252    Pyr      CH═CH 2-NH.sub.2 -4-Thiazo                              1-253    Pyr      CH═CH 2-AcNH-4-Thiazo                                   1-254    Pyr      CH═CH 4,5-diMe-2-Thiazo                                 1-255    Pyr      CH═CH 2-HO-5-Me-4-Thiazo                                1-256    Pyr      CH═CH 5-NH.sub.2 -2-Me-4-Thiazo                         1-257    Pyr      CH═CH 3-Isothiazo                                       1-258    Pyr      CH═CH 4-Isothiazo                                       1-259    Pyr      CH═CH 3-Pyrazo                                          1-260    Pyr      CH═CH 4-Pyrazo                                          1-261    Pyr      CH═CH 1-Me-3-Pyrazo                                     1-262    Pyr      CH═CH 1-Et-3-Pyrazo                                     1-263    Pyr      CH═CH 1-Me-4-Pyrazo                                     1-264    Pyr      CH═CH 1-Et-4-Pyrazo                                     1-265    Pyr      CH═CH 4-Me-3-Pyrazo                                     1-266    Pyr      CH═CH 5-Me-3-Pyrazo                                     1-267    Pyr      CH═CH 5-Me-4-Pyrazo                                     1-268    Pyr      CH═CH 4-MeO-3-Pyrazo                                    1-269    Pyr      CH═CH 4-HO-3-Pyrazo                                     1-270    Pyr      CH═CH 4-Cl-3-Pyrazo                                     1-271    Pyr      CH═CH 4-NH.sub.2 -3-Pyrazo                              1-272    Pyr      CH═CH 5-NH.sub.2 -3-Pyrazo                              1-273    Pyr      CH═CH 3-NH.sub.2 -4-Pyrazo                              1-274    Pyr      CH═CH 4-AcNH-3-Pyrazo                                   1-275    Pyr      CH═CH 5-Ph-3-Pyrazo                                     1-276    Pyr      CH═CH 1,5-diMe-3-Pyrazo                                 1-277    Pyr      CH═CH 1,4-diMe-3-Pyrazo                                 1-278    Pyr      CH═CH 3,5-diMe-4-Pyrazo                                 1-279    Pyr      CH═CH 1,5-diMe-4-Pyrazo                                 1-280    Pyr      CH═CH 1,3-diMe-4-Pyrazo                                 1-281    Pyr      CH═CH 1,3-diMe-5-Pyrazo                                 1-282    Pyr      CH═CH 3-Cl-5-Me-4-Pyrazo                                1-283    Pyr      CH═CH 3-Cl-1-Me-4-Pyrazo                                1-284    Pyr      CH═CH 4-Cl-5-Me-3-Pyrazo                                1-285    Pyr      CH═CH 4-Cl-1-Me-3-Pyrazo                                1-286    Pyr      CH═CH 3-NH.sub.2 -5-Me-4-Pyrazo                         1-287    Pyr      CH═CH 3-NH.sub.2 -1-Me-4-Pyrazo                         1-288    Pyr      CH═CH 5-NH.sub.2 -1-Me-4-Pyrazo                         1-289    Pyr      CH═CH 5-NH.sub.2 -4-Me-3-Pyrazo                         1-290    Pyr      CH═CH 5-NH.sub.2 -1-Me-3-Pyrazo                         1-291    Pyr      CH═CH 5-NH.sub.2 -3-Me-3-Pyrazo                         1-292    Pyr      CH═CH 4-NH.sub.2 -5-Me-3-Pyrazo                         1-293    Pyr      CH═CH 4-HO-5-Me-3-Pyrazo                                1-294    Pyr      CH═CH 1,3,5-triMe-4-Pyrazo                              1-295    Pyr      CH═CH 1,3,4-triMe-5-Pyrazo                              1-296    Pyr      CH═CH 4-Cl-1,3-diMe-5-Pyrazo                            1-297    Pyr      CH═CH 2-Imidazo                                         1-298    Pyr      CH═CH 4-Imidazo                                         1-299    Pyr      CH═CH 1-Me-4-Imidazo                                    1-300    Pyr      CH═CH 5-Me-4-Imidazo                                    1-301    Pyr      CH═CH 5-Me-2-Imidazo                                    1-302    Pyr      CH═CH 1-Me-2-Imidazo                                    1-303    Pyr      CH═CH 1,2,3-Oxadiazo-5-yl                               1-304    Pyr      CH═CH 1,2,4-Oxadiazo-5-yl                               1-305    Pyr      CH═CH 1,2,5-Oxadiazo-3-yl                               1-306    Pyr      CH═CH 5-Me-1,2,3-Oxadiazo-4-yl                          1-307    Pyr      CH═CH 1,2,3-Thiadiazo-4-yl                              1-308    Pyr      CH═CH 1,2,4-Thiadiazo-2-yl                              1-309    Pyr      CH═CH 1,2,5-Thiadiazo-3-yl                              1-310    Pyr      CH═CH 4-Me-1,2,3-Thiadiazo-5-yl                         1-311    Pyr      CH═CH 5-Ph-1,2,3-Thiadiazo-4-yl                         1-312    NMe.sub.2                                                                              CH═CH 2-Fur                                             1-313    NMe.sub.2                                                                              CH═CH 3-Fur                                             1-314    NMe.sub.2                                                                              CH═CH 4-Me-2-Fur                                        1-315    NMe.sub.2                                                                              CH═CH 2,4-diMe-3-Fur                                    1-316    NMe.sub.2                                                                              CH═CH 2-Thi                                             1-317    NMe.sub.2                                                                              CH═CH 3-Thi                                             1-318    NMe.sub.2                                                                              CH═CH 3-Me-2-Thi                                        1-319    NMe.sub.2                                                                              CH═CH 2-Me-3-Thi                                        1-320    NMe.sub.2                                                                              CH═CH 4,5-diMe-2-Thi                                    1-321    NMe.sub.2                                                                              CH═CH 2-Pyl                                             1-322    NMe.sub.2                                                                              CH═CH 3-Pyl                                             1-323    NMe.sub.2                                                                              CH═CH 1-Me-2-Pyl                                        1-324    NMe.sub.2                                                                              CH═CH 4-Me-2-Pyl                                        1-325    NMe.sub.2                                                                              CH═CH 2-Me-3-Pyl                                        1-326    NMe.sub.2                                                                              CH═CH 3,5-diMe-2-Pyl                                    1-327    NMe.sub.2                                                                              CH═CH 1,3-diMe-2-Pyl                                    1-328    NMe.sub.2                                                                              CH═CH 4-Oxazo                                           1-329    NMe.sub.2                                                                              CH═CH 5-Oxazo                                           1-330    NMe.sub.2                                                                              CH═CH 2-Oxazo                                           1-331    NMe.sub.2                                                                              CH═CH 2-Me-4-Oxazo                                      1-332    NMe.sub.2                                                                              CH═CH 2,5-diMe-4-Oxazo                                  1-333    NMe.sub.2                                                                              CH═CH 3-Isoxazo                                         1-334    NMe.sub.2                                                                              CH═CH 4-Isoxazo                                         1-335    NMe.sub.2                                                                              CH═CH 5-Me-3-Isoxazo                                    1-336    NMe.sub.2                                                                              CH═CH 4-MeO-3-Isoxazo                                   1-337    NMe.sub.2                                                                              CH═CH 4-HO-3-Isoxazo                                    1-338    NMe.sub.2                                                                              CH═CH 4,5-diMe-3-Isoxazo                                1-339    NMe.sub.2                                                                              CH═CH 4-HO-5-Me-3-Isoxzo                                1-340    NMe.sub.2                                                                              CH═CH 2-Thiazo                                          1-341    NMe.sub.2                                                                              CH═CH 4-Thiazo                                          1-342    NMe.sub.2                                                                              CH═CH 5-Thiazo                                          1-343    NMe.sub.2                                                                              CH═CH 4-Me-2-Thiazo                                     1-344    NMe.sub.2                                                                              CH═CH 2-Me-5-Thiazo                                     1-345    NMe.sub.2                                                                              CH═CH 2-MeO-4-Thiazo                                    1-346    NMe.sub.2                                                                              CH═CH 4,5-diMe-2-Thiazo                                 1-347    NMe.sub.2                                                                              CH═CH 3-Isothiazo                                       1-348    NMe.sub.2                                                                              CH═CH 4-Isothiazo                                       1-349    NMe.sub.2                                                                              CH═CH 3-Pyrazo                                          1-350    NMe.sub.2                                                                              CH═CH 4-Pyrazo                                          1-351    NMe.sub.2                                                                              CH═CH 1-Me-3-Pyrazo                                     1-352    NMe.sub.2                                                                              CH═CH 1-Me-4-Pyrazo                                     1-353    NMe.sub.2                                                                              CH═CH 4-Me-3-Pyrazo                                     1-354    NMe.sub.2                                                                              CH═CH 5-Me-3-Pyrazo                                     1-355    NMe.sub.2                                                                              CH═CH 5-Me-4-Pyrazo                                     1-356    NMe.sub.2                                                                              CH═CH 4-MeO-3-Pyrazo                                    1-357    NMe.sub.2                                                                              CH═CH 4-HO-3-Pyrazo                                     1-358    NMe.sub.2                                                                              CH═CH 3,5-diMe-4-Pyrazo                                 1-359    NMe.sub.2                                                                              CH═CH 1,3,5-triMe-4-Pyrazo                              1-360    NMe.sub.2                                                                              CH═CH 1,3,4-triMe-5-Pyrazo                              1-361    NMe.sub.2                                                                              CH═CH 2-Imidazo                                         1-362    NMe.sub.2                                                                              CH═CH 4-Imidazo                                         1-363    NMe.sub.2                                                                              CH═CH 5-Me-4-Imidazo                                    1-364    Azi      CH═CH 2-Fur                                             1-365    Azi      CH═CH 3-Fur                                             1-366    Azi      CH═CH 4-Me-2-Fur                                        1-367    Azi      CH═CH 2-Thi                                             1-368    Azi      CH═CH 3-Thi                                             1-369    Azi      CH═CH 5-Me-2-Thi                                        1-370    Azi      CH═CH 2-Pyl                                             1-371    Azi      CH═CH 3-Pyl                                             1-372    Azi      CH═CH 1-Me-2-Pyl                                        1-373    Azi      CH═CH 4-Me-2-Pyl                                        1-374    Azi      CH═CH 4-Oxazo                                           1-375    Azi      CH═CH 5-Oxazo                                           1-376    Azi      CH═CH 2-Oxazo                                           1-377    Azi      CH═CH 3-Isoxazo                                         1-378    Azi      CH═CH 4-Isoxazo                                         1-379    Azi      CH═CH 4-HO-3-Isoxazo                                    1-380    Azi      CH═CH 2-Thiazo                                          1-381    Azi      CH═CH 4-Thiazo                                          1-382    Azi      CH═CH 5-Thiazo                                          1-383    Azi      CH═CH 2-Me-5-Thiazo                                     1-384    Azi      CH═CH 3-Pyrazo                                          1-385    Azi      CH═CH 4-Pyrazo                                          1-386    Azi      CH═CH 1-Me-3-Pyrazo                                     1-387    Azi      CH═CH 4-Me-3-Pyrazo                                     1-388    Azi      CH═CH 5-Me-4-Pyrazo                                     1-389    Azi      CH═CH 4-NH.sub.2 -3-Pyrazo                              1-390    Azi      CH═CH 3-NH.sub.2 -4-Pyrazo                              1-391    Azi      CH═CH 3,5-diMe-4-Pyrazo                                 1-392    Azi      CH═CH 1,3,5-triMe-4-Pyrazo                              1-393    Azi      CH═CH 2-Imidazo                                         1-394    Azi      CH═CH 4-Imidazo                                         1-395    Azi      CH═CH 5-Me-4-Imidazo                                    1-396    Aze      CH═CH 2-Fur                                             1-397    Aze      CH═CH 3-Fur                                             1-398    Aze      CH═CH 4-Me-2-Fur                                        1-399    Aze      CH═CH 2-Thi                                             1-400    Aze      CH═CH 3-Thi                                             1-401    Aze      CH═CH 5-Me-2-Thi                                        1-402    Aze      CH═CH 2-Pyl                                             1-403    Aze      CH═CH 3-Pyl                                             1-404    Aze      CH═CH 1-Me-2-Pyl                                        1-405    Aze      CH═CH 4-Me-2-Pyl                                        1-406    Aze      CH═CH 4-Oxazo                                           1-407    Aze      CH═CH 5-Oxazo                                           1-408    Aze      CH═CH 2-Oxazo                                           1-409    Aze      CH═CH 3-Isoxazo                                         1-410    Aze      CH═CH 4-Isoxazo                                         1-411    Aze      CH═CH 4-HO-3-Isoxazo                                    1-412    Aze      CH═CH 2-Thiazo                                          1-413    Aze      CH═CH 4-Thiazo                                          1-414    Aze      CH═CH 5-Thiazo                                          1-415    Aze      CH═CH 2-Me-5-Thiazo                                     1-416    Aze      CH═CH 3-Pyrazo                                          1-417    Aze      CH═CH 4-Pyrazo                                          1-418    Aze      CH═CH 1-Me-3-Pyrazo                                     1-419    Aze      CH═CH 4-Me-3-Pyrazo                                     1-420    Aze      CH═CH 5-Me-4-Pyrazo                                     1-421    Aze      CH═CH 4-NH2 -3-Pyrazo                                   1-422    Aze      CH═CH 3-NH2 -4-Pyrazo                                   1-423    Aze      CH═CH 3,5-diMe-4-Pyrazo                                 1-424    Aze      CH═CH 1,3,5-triMe-4-Pyrazo                              1-425    Aze      CH═CH 2-Imidazo                                         1-426    Aze      CH═CH 4-Imidazo                                         1-427    Aze      CH═CH 5-Me-4-Imidazo                                    1-428    Pip      CH═CH 1,2,3-Triazo-4-yl                                 1-429    Pip      CH═CH 1-Me-1,2,3-Triazo-4-yl                            1-430    Pip      CH═CH 5-Me-1,2,3-Triazo-4-yl                            1-431    Pip      CH═CH 1,5-diMe-1,2,3-Triazo-4-yl                        1-432    Pip      CH═CH 1,2,4-Triazo-5-yl                                 1-433    Pip      CH═CH 1-Me-1,2,5-Triazo-3-yl                            1-434    Pyr      CH═CH 1,2,3-Triazo-4-yl                                 1-435    Pyr      CH═CH 1,2,4-Triazo-5-yl                                 1-436    NMe.sub.2                                                                              CH═CH 1,2,3-Triazo-4-yl                                 1-437    NMe.sub.2                                                                              CH═CH 1,2,4-Triazo-5-yl                                 1-438    Pip      (CH.sub.2).sub.3                                                                        2-Fur                                             1-439    Pip      (CH.sub.2).sub.3                                                                        3-Fur                                             1-440    Pip      (CH.sub.2).sub.3                                                                        4-Me-2-Fur                                        1-441    Pip      (CH.sub.2).sub.3                                                                        2-Thi                                             1-442    Pip      (CH.sub.2).sub.3                                                                        3-Thi                                             1-443    Pip      (CH.sub.2).sub.3                                                                        5-Me-2-Thi                                        1-444    Pip      (CH.sub.2).sub.3                                                                        2-Pyl                                             1-445    Pip      (CH.sub.2).sub.3                                                                        3-Pyl                                             1-446    Pip      (CH.sub.2).sub.3                                                                        1-Me-2-Pyl                                        1-447    Pip      (CH.sub.2).sub.3                                                                        4-Me-2-Pyl                                        1-448    Pip      (CH.sub.2).sub.3                                                                        3,5-diMe-2-Pyl                                    1-449    Pip      (CH.sub.2).sub.3                                                                        4-Oxazo                                           1-450    Pip      (CH.sub.2).sub.3                                                                        5-Oxazo                                           1-451    Pip      (CH.sub.2).sub.3                                                                        2-Oxazo                                           1-452    Pip      (CH.sub.2).sub.3                                                                        2-Me-4-Oxazo                                      1-453    Pip      (CH.sub.2).sub.3                                                                        3-Isoxazo                                         1-454    Pip      (CH.sub.2).sub.3                                                                        4-Isoxazo                                         1-455    Pip      (CH.sub.2).sub.3                                                                        5-Me-3-Isoxazo                                    1-456    Pip      (CH.sub.2).sub.3                                                                        4-HO-3-Isoxazo                                    1-457    Pip      (CH.sub.2).sub.3                                                                        2-Thiazo                                          1-458    Pip      (CH.sub.2).sub.3                                                                        4-Thiazo                                          1-459    Pip      (CH.sub.2).sub.3                                                                        5-Thiazo                                          1-460    Pip      (CH.sub.2).sub.3                                                                        2-Me-5-Thiazo                                     1-461    Pip      (CH.sub.2).sub.3                                                                        3-Pyrazo                                          1-462    Pip      (CH.sub.2).sub.3                                                                        4-Pyrazo                                          1-463    Pip      (CH.sub.2).sub.3                                                                        1-M.e-3-Pyrazo                                    1-464    Pip      (CH.sub.2).sub.3                                                                        1-Me-4-Pyrazo                                     1-465    Pip      (CH.sub.2).sub.3                                                                        4-Me-3-Pyrazo                                     1-466    Pip      (CH.sub.2).sub.3                                                                        5-Me-3-Pyrazo                                     1-467    Pip      (CH.sub.2).sub.3                                                                        5-Me-4-Pyrazo                                     1-468    Pip      (CH.sub.2).sub.3                                                                        4-NH.sub.2 -3-Pyrazo                              1-469    Pip      (CH.sub.2).sub.3                                                                        5-NH.sub.2 -3-Pyrazo                              1-470    Pip      (CH.sub.2).sub.3                                                                        3-NH.sub.2 -4-Pyrazo                              1-471    Pip      (CH.sub.2).sub.3                                                                        3,5-diMe-4-Pyrazo                                 1-472    Pip      (CH.sub.2).sub.3                                                                        1,3,5-triMe-4-Pyrazo                              1-473    Pip      (CH.sub.2).sub.3                                                                        2-Imidazo                                         1-474    Pip      (CH.sub.2).sub.3                                                                        4-Imidazo                                         1-475    Pip      (CH.sub.2).sub.3                                                                        5-Me-4-Imidazo                                    1-476    Pip      CH.sub.2 CH.sub.2                                                                       2-Fur                                             1-477    Pip      CH.sub.2 CH.sub.2                                                                       3-Fur                                             1-478    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-2-Fur                                        1-479    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-2-Fur                                        1-480    Pip      CH.sub.2 CH.sub.2                                                                       2-Me-3-Fur                                        1-481    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-3-Fur                                        1-482    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-2-Fur                                        1-483    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-3-Fur                                        1-484    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -2-Fur                                 1-485    Pip      CH.sub.2 CH.sub.2                                                                       5-AcNH-2-Fur                                      1-486    Pip      CH.sub.2 CH.sub.2                                                                       5-Ph-2-Fur                                        1-487    Pip      CH.sub.2 CH.sub.2                                                                       5-(4-MePh)-2-Fur                                  1-488    Pip      CH.sub.2 CH.sub.2                                                                       5-(4-ClPh)-2-Fur                                  1-489    Pip      CH.sub.2 CH.sub.2                                                                       3-Me-5-NH.sub.2 -2-Fur                            1-490    Pip      CH.sub.2 CH.sub.2                                                                       2,4-diMe-3-Fur                                    1-491    Pip      CH.sub.2 CH.sub.2                                                                       2-Thi                                             1-492    Pip      CH.sub.2 CH.sub.2                                                                       3-Thi                                             1-493    Pip      CH.sub.2 CH.sub.2                                                                       3-Me-2-Thi                                        1-494    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-2-Thi                                        1-495    Pip      CH.sub.2 CH.sub.2                                                                       2-Me-3-Thi                                        1-496    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-3-Thi                                        1-497    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-3-Thi                                        1-498    Pip      CH.sub.2 CH.sub.2                                                                       4-MeO-2-Thi                                       1-499    Pip      CH.sub.2 CH.sub.2                                                                       4-MeO-3-Thi                                       1-500    Pip      CH.sub.2 CH.sub.2                                                                       4-HO-2-Thi                                        1-501    Pip      CH.sub.2 CH.sub.2                                                                       4-HO-3-Thi                                        1-502    Pip      CH.sub.2 CH.sub.2                                                                       5-Et-2-Thi                                        1-503    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-2-Thi                                        1-504    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-3-Thi                                        1-505    Pip      CH.sub.2 CH.sub.2                                                                       5-Br-3-Thi                                        1-506    Pip      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -2-Thi                                 1-507    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -2-Thi                                 1-508    Pip      CH.sub.2 CH.sub.2                                                                       2-NH.sub.2 -3-Thi                                 1-509    Pip      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3-Thi                                 1-510    Pip      CH.sub.2 CH.sub.2                                                                       3-AcNH-2-Thi                                      1-511    Pip      CH.sub.2 CH.sub.2                                                                       4-AcNH-3-Thi                                      1-512    Pip      CH.sub.2 CH.sub.2                                                                       5-Ph-2-Thi                                        1-513    Pip      CH.sub.2 CH.sub.2                                                                       4,5-diMe-2-Thi                                    1-514    Pip      CH.sub.2 CH.sub.2                                                                       3,5-diMe-2-Thi                                    1-515    Pip      CH.sub.2 CH.sub.2                                                                       2,5-diMe-3-Thi                                    1-516    Pip      CH.sub.2 CH.sub.2                                                                       4,5-diMe-3-Thi                                    1-517    Pip      CH.sub.2 CH.sub.2                                                                       4,5-diCl-2-Thi                                    1-518    Pip      CH.sub.2 CH.sub.2                                                                       2-NH.sub.2 -5-Ph-3-Thi                            1-519    Pip      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -2,5-diMe-3-Thi                        1-520    Pip      CH.sub.2 CH.sub.2                                                                       2-Pyl                                             1-521    Pip      CH.sub.2 CH.sub.2                                                                       3-Pyl                                             1-522    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-2-Pyl                                        1-523    Pip      CH.sub.2 CH.sub.2                                                                       3-Me-2-Pyl                                        1-524    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-2-Pyl                                        1-525    Pip      CH.sub.2 CH.sub.2                                                                       2-Me-3-Pyl                                        1-526    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-3-Pyl                                        1-527    Pip      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -2-Pyl                                 1-528    Pip      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -2-Pyl                                 1-529    Pip      CH.sub.2 CH.sub.2                                                                       3-AcNH-2-Pyl                                      1-530    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-2-Pyl                                        1-531    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-3-Pyl                                        1-532    Pip      CH.sub.2 CH.sub.2                                                                       4-Ph-2-Pyl                                        1-533    Pip      CH.sub.2 CH.sub.2                                                                       5-Ph-3-Pyl                                        1-534    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-4-MeO-3-pyl                                  1-535    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-4-HO-3-Pyl                                   1-536    Pip      CH.sub.2 CH.sub.2                                                                       3,5-diMe-2-Pyl                                    1-537    Pip      CH.sub.2 CH.sub.2                                                                       4,5-diMe-2-Pyl                                    1-538    Pip      CH.sub.2 CH.sub.2                                                                       1,3-diMe-2-Pyl                                    1-539    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -1-Me-2-Pyl                            1-540    Pip      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3,5-diMe-2-Pyl                        1-541    Pip      CH.sub.2 CH.sub.2                                                                       5-Br-1,4-diMe-3-Pyl                               1-542    Pip      CH.sub.2 CH.sub.2                                                                       4-Oxazo                                           1-543    Pip      CH.sub.2 CH.sub.2                                                                       5-Oxazo                                           1-544    Pip      CH.sub.2 CH.sub.2                                                                       2-Oxazo                                           1-545    Pip      CH.sub.2 CH.sub.2                                                                       2-Me-4-Oxazo                                      1-546    Pip      CH.sub.2 CH.sub.2                                                                       2-Ph-4-Oxazo                                      1-547    Pip      CH.sub.2 CH.sub.2                                                                       5-Ph-2-Oxazo                                      1-548    Pip      CH.sub.2 CH.sub.2                                                                       2-HO-4-Oxazo                                      1-549    Pip      CH.sub.2 CH.sub.2                                                                       2,5-diMe-4-Oxazo                                  1-550    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-2-Ph-5-Oxazo                                 1-551    Pip      CH.sub.2 CH.sub.2                                                                       3-Isoxazo                                         1-552    Pip      CH.sub.2 CH.sub.2                                                                       4-Isoxazo                                         1-553    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-3-Isoxazo                                    1-554    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-3-Isoxazo                                    1-555    Pip      CH.sub.2 CH.sub.2                                                                       3-Me-4-Isoxazo                                    1-556    Pip      CH.sub.2 CH.sub.2                                                                       4-MeO-3-Isoxazo                                   1-557    Pip      CH.sub.2 CH.sub.2                                                                       4-HO-3-Isoxazo                                    1-558    Pip      CH.sub.2 CH.sub.2                                                                       3-HO-4-Isoxazo                                    1-559    Pip      CH.sub.2 CH.sub.2                                                                       3-HO-5-Isoxazo                                    1-560    Pip      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3-Isoxazo                             1-561    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -4-Isoxazo                             1-562    Pip      CH.sub.2 CH.sub.2                                                                       5-Ph-3-Isoxazo                                    1-563    Pip      CH.sub.2 CH.sub.2                                                                       4-Ph-3-Isoxazo                                    1-564    Pip      CH.sub.2 CH.sub.2                                                                       4,5-diMe-3-Isoxazo                                1-565    Pip      CH.sub.2 CH.sub.2                                                                       4-HO-5-Me-3-Isoxazo                               1-566    Pip      CH.sub.2 CH.sub.2                                                                       2-Thiazo                                          1-567    Pip      CH.sub.2 CH.sub.2                                                                       4-Thiazo                                          1-568    Pip      CH.sub.2 CH.sub.2                                                                       5-Thiazo                                          1-569    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-2-Thiazo                                     1-570    Pip      CH.sub.2 CH.sub.2                                                                       2-Me-4-Thiazo                                     1-571    Pip      CH.sub.2 CH.sub.2                                                                       2-Me-5-Thiazo                                     1-572    Pip      CH.sub.2 CH.sub.2                                                                       2-MeO-4-Thiazo                                    1-573    Pip      CH.sub.2 CH.sub.2                                                                       2-MeO-5-Thiazo                                    1-574    Pip      CH.sub.2 CH.sub.2                                                                       2-HO-4-Thiazo                                     1-575    Pip      CH.sub.2 CH.sub.2                                                                       2-HO-5-Thiazo                                     1-576    Pip      CH.sub.2 CH.sub.2                                                                       2-Cl-5-Thiazo                                     1-577    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-2-Thiazo                                     1-578    Pip      CH.sub.2 CH.sub.2                                                                       2-NH 4-Thiazo                                     1-579    Pip      CH.sub.2 CH.sub.2                                                                       2-NH.sub.2 -5-Thiazo                              1-580    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -4-Thiazo                              1-581    Pip      CH.sub.2 CH.sub.2                                                                       2-AcNH-4-Thiazo                                   1-582    Pip      CH.sub.2 CH.sub.2                                                                       5-AcNH-4-Thiazo                                   1-583    Pip      CH.sub.2 CH.sub.2                                                                       2-Ph-4-Thiazo                                     1-584    Pip      CH.sub.2 CH.sub.2                                                                       4,5-diMe-2-Thiazo                                 1-585    Pip      CH.sub.2 CH.sub.2                                                                       2-HO-5-Me-4-Thiazo                                1-586    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -2-Me-4-Thiazo                         1-587    Pip      CH.sub.2 CH.sub.2                                                                       2-Cl-4-Me-5-Thiazo                                1-588    Pip      CH.sub.2 CH.sub.2                                                                       3-Isothiazo                                       1-589    Pip      CH.sub.2 CH.sub.2                                                                       4-Isothiazo                                       1-590    Pip      CH.sub.2 CH.sub.2                                                                       3-Pyrazo                                          1-591    Pip      CH.sub.2 CH.sub.2                                                                       4-Pyrazo                                          1-592    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-3-Pyrazo                                     1-593    Pip      CH.sub.2 CH.sub.2                                                                       1-Et-3-Pyrazo                                     1-594    Pip      CH.sub.2 CH.sub.2                                                                       1-Pr-3-Pyrazo                                     1-595    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-4-Pyrazo                                     1-596    Pip      CH.sub.2 CH.sub.2                                                                       1-Et-4-Pyrazo                                     1-597    Pip      CH.sub.2 CH.sub.2                                                                       1-Pr-4-Pyrazo                                     1-598    Pip      CH.sub.2 CH.sub.2                                                                       1-Bu-4-Pyrazo                                     1-599    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-3-Pyrazo                                     1-600    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-3-Pyrazo                                     1-601    Pip      CH.sub.2 CH.sub.2                                                                       5-Et-3-Pyrazo                                     1-602    Pip      CH.sub.2 CH.sub.2                                                                       5-Pr-3-Pyrazo                                     1-603    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-4-Pyrazo                                     1-604    Pip      CH.sub.2 CH.sub.2                                                                       4-MeO-3-Pyrazo                                    1-605    Pip      CH.sub.2 CH.sub.2                                                                       4-PrO-3-Pyrazo                                    1-606    Pip      CH.sub.2 CH.sub.2                                                                       4-HO-3-Pyrazo                                     1-607    Pip      CH.sub.2 CH.sub.2                                                                       4-Cl-3-Pyrazo                                     1-608    Pip      CH.sub.2 CH.sub.2                                                                       4-Br-3-Pyrazo                                     1-609    Pip      CH.sub.2 CH.sub.2                                                                       3-Cl-4-Pyrazo                                     1-610    Pip      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3-Pyrazo                              1-611    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -3-Pyrazo                              1-612    Pip      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -4-Pyrazo                              1-613    Pip      CH.sub.2 CH.sub.2                                                                       4-AcNH-3-Pyrazo                                   1-614    Pip      CH.sub.2 CH.sub.2                                                                       5-AcNH-3-Pyrazo                                   1-615    Pip      CH.sub.2 CH.sub.2                                                                       3-AcNH-4-Pyrazo                                   1-616    Pip      CH.sub.2 CH.sub.2                                                                       3-EtCONH-4-Pyrazo                                 1-617    Pip      CH.sub.2 CH.sub.2                                                                       5-Ph-3-Pyrazo                                     1-618    Pip      CH.sub.2 CH.sub.2                                                                       1,5-diMe-3-Pyrazo                                 1-619    Pip      CH.sub.2 CH.sub.2                                                                       1,4-diMe-3-Pyrazo                                 1-620    Pip      CH.sub.2 CH.sub.2                                                                       4,5-diMe-3-Pyrazo                                 1-621    Pip      CH.sub.2 CH.sub.2                                                                       3-Me-4-Pyrazo                                     1-622    Pip      CH.sub.2 CH.sub.2                                                                       3,5-diMe-4-Pyrazo                                 1-623    Pip      CH.sub.2 CH.sub.2                                                                       1,5-diMe-4-Pyrazo                                 1-624    Pip      CH.sub.2 CH.sub.2                                                                       1,3-diMe-4-Pyrazo                                 1-625    Pip      CH.sub.2 CH.sub.2                                                                       1,3-diMe-5-Pyrazo                                 1-626    Pip      CH.sub.2 CH.sub.2                                                                       3-Cl-5-Me-4-Pyrazo                                1-627    Pip      CH.sub.2 CH.sub.2                                                                       3-Cl-1-Me-4-Pyrazo                                1-628    Pip      CH.sub.2 CH.sub.2                                                                       5-Cl-1-Me-4-Pyrazo                                1-629    Pip      CH.sub.2 CH.sub.2                                                                       4-Cl-1-Me-3-Pyrazo                                1-630    Pip      CH.sub.2 CH.sub.2                                                                       4-Cl-5-Me-3-Pyrazo                                1-631    Pip      CH.sub.2 CH.sub.2                                                                       4-Cl-1-Me-3-Pyrazo                                1-632    Pip      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -5-Me-4-Pyrazo                         1-633    Pip      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -1-Me-4-Pyrazo                         1-634    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -1-Me-4-Pyrazo                         1-635    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -4-Me-3-Pyrazo                         1-636    Pip      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -1-Me-3-Pyrazo                         1-637    Pip      CH.sub.2 CH.sub.2                                                                       5-AcNH-1-Me-4-Pyrazo                              1-638    Pip      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -5-Me-3-Pyrazo                         1-639    Pip      CH.sub.2 CH.sub.2                                                                       4-HO-5-Me-3-Pyrazo                                1-640    Pip      CH.sub.2 CH.sub.2                                                                       5-AcNH-3-Me-4-Pyrazo                              1-641    Pip      CH.sub.2 CH.sub.2                                                                       1,3,5-triMe-4-Pyrazo                              1-642    Pip      CH.sub.2 CH.sub.2                                                                       1,3,4-triMe-5-Pyrazo                              1-643    Pip      CH.sub.2 CH.sub.2                                                                       4-Cl-1,3-diMe-5-Pyrazo                            1-644    Pip      CH.sub.2 CH.sub.2                                                                       2-Imidazo                                         1-645    Pip      CH.sub.2 CH.sub.2                                                                       4-Imidazo                                         1-646    Pip      CH.sub.2 CH.sub.2                                                                       2-Me-4-Imidazo                                    1-647    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-4-Imidazo                                    1-648    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-4-Imidazo                                    1-649    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-2-Imidazo                                    1-650    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-2-Imidazo                                    1-651    Pip      CH.sub.2 CH.sub.2                                                                       1,2,3-Oxadiazo-5-yl                               1-652    Pip      CH.sub.2 CH.sub.2                                                                       1,3,4-Oxadiazo-2-yl                               1-653    Pip      CH.sub.2 CH.sub.2                                                                       1,2,3-Oxadiazo-4-yl                               1-654    Pip      CH.sub.2 CH.sub.2                                                                       1,2,4-Oxadiazo-5-yl                               1-655    Pip      CH.sub.2 CH.sub.2                                                                       1,2,4-Oxadiazo-3-yl                               1-656    Pip      CH.sub.2 CH.sub.2                                                                       1,2,5-Oxadiazo-3-yl                               1-657    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-1,2,3-Oxadiazo-4-yl                          1-658    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-1,2,5-Oxadiazo-3-yl                          1-659    Pip      CH.sub.2 CH.sub.2                                                                       4-Ph-1,2,5-Oxadiazo-3-yl                          1-660    Pip      CH.sub.2 CH.sub.2                                                                       1,2,3-Thiadiazo-4-yl                              1-661    Pip      CH.sub.2 CH.sub.2                                                                       1,2,3-Thiadiazo-5-yl                              1-662    Pip      CH.sub.2 CH.sub.2                                                                       1,3,4-Thiadiazo-2-yl                              1-663    Pip      CH.sub.2 CH.sub.2                                                                       1,2,4-Thiadiazo-3-yl                              1-664    Pip      CH.sub.2 CH.sub.2                                                                       1,2,4-Thiadiazo-5-yl                              1-665    Pip      CH.sub.2 CH.sub.2                                                                       1,2,5-Thiadiazo-3-yl                              1-666    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-1,2,3-Thiadiazo-5-yl                         1-667    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-1,2,3-Thiadiazo-4-yl                         1-668    Pip      CH.sub.2 CH.sub.2                                                                       4-Me-1,2,5-Thiadiazo-3-yl                         1-669    Pip      CH.sub.2 CH.sub.2                                                                       5-Ph-1,2,3-Thiadiazo-4-yl                         1-670    Pyr      CH.sub.2 CH.sub.2                                                                       2-Fur                                             1-671    Pyr      CH.sub.2 CH.sub.2                                                                       3-Fur                                             1-672    Pyr      CH.sub.2 CH.sub.2                                                                       4-Me-2-Fur                                        1-673    Pyr      CH.sub.2 CH.sub.2                                                                       2-Me-3-Fur                                        1-674    Pyr      CH.sub.2 CH.sub.2                                                                       2,4-diMe-3-Fur                                    1-675    Pyr      CH.sub.2 CH.sub.2                                                                       2-Thi                                             1-676    Pyr      CH.sub.2 CH.sub.2                                                                       3-Thi                                             1-677    Pyr      CH.sub.2 CH.sub.2                                                                       3-Me-2-Thi                                        1-678    Pyr      CH.sub.2 CH.sub.2                                                                       2-Me-3-Thi                                        1-679    Pyr      CH.sub.2 CH.sub.2                                                                       4-Me-3-Thi                                        1-680    Pyr      CH.sub.2 CH.sub.2                                                                       4-MeO-3-Thi                                       1-681    Pyr      CH.sub.2 CH.sub.2                                                                       4-HO-2-Thi                                        1-682    Pyr      CH.sub.2 CH.sub.2                                                                       5-Cl-3-Thi                                        1-683    Pyr      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -2-Thi                                 1-684    Pyr      CH.sub.2 CH.sub.2                                                                       2-NH.sub.2 -3-Thi                                 1-685    Pyr      CH.sub.2 CH.sub.2                                                                       3-AcNH-2-Thi                                      1-686    Pyr      CH.sub.2 CH.sub.2                                                                       5-Ph-2-Thi                                        1-687    Pyr      CH.sub.2 CH.sub.2                                                                       4,5-diMe-2-Thi                                    1-688    Pyr      CH.sub.2 CH.sub.2                                                                       2,5-diMe-3-Thi                                    1-689    Pyr      CH.sub.2 CH.sub.2                                                                       4,5-diCl-2-Thi                                    1-690    Pyr      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -2,5-diMe-3-Thi                        1-691    Pyr      CH.sub.2 CH.sub.2                                                                       2-Pyl                                             1-692    Pyr      CH.sub.2 CH.sub.2                                                                       3-Pyl                                             1-693    Pyr      CH.sub.2 CH.sub.2                                                                       1-Me-2-Pyl                                        1-694    Pyr      CH.sub.2 CH.sub.2                                                                       3-Me-2-Pyl                                        1-695    Pyr      CH.sub.2 CH.sub.2                                                                       4-Me-2-Pyl                                        1-696    Pyr      CH.sub.2 CH.sub.2                                                                       2-Me-3-Pyl                                        1-697    Pyr      CH.sub.2 CH.sub.2                                                                       1-Me-4-MeO-3-Pyl                                  1-698    Pyr      CH.sub.2 CH.sub.2                                                                       1-Me-4-HO-3-Pyl                                   1-699    Pyr      CH.sub.2 CH.sub.2                                                                       3,5-diMe-2-Pyl                                    1-700    Pyr      CH.sub.2 CH.sub.2                                                                       1,3-diMe-2-Pyl                                    1-701    Pyr      CH.sub.2 CH.sub.2                                                                       4-Oxazo                                           1-702    Pyr      CH.sub.2 CH.sub.2                                                                       5-Oxazo                                           1-703    Pyr      CH.sub.2 CH.sub.2                                                                       2-Oxazo                                           1-704    Pyr      CH.sub.2 CH.sub.2                                                                       2-Me-4-Oxazo                                      1-705    Pyr      CH.sub.2 CH.sub.2                                                                       5-Ph-2-Oxazo                                      1-706    Pyr      CH.sub.2 CH.sub.2                                                                       2,5-d.iMe-4-Oxazo                                 1-707    Pyr      CH.sub.2 CH.sub.2                                                                       3-Isoxazo                                         1-708    Pyr      CH.sub.2 CH.sub.2                                                                       4-Isoxazo                                         1-709    Pyr      CH.sub.2 CH.sub.2                                                                       5-Me-3-Isoxazo                                    1-710    Pyr      CH.sub.2 CH.sub.2                                                                       3-Me-4-Isoxazo                                    1-711    Pyr      CH.sub.2 CH.sub.2                                                                       4-MeO-3-Isoxazo                                   1-712    Pyr      CH.sub.2 CH.sub.2                                                                       4-HO-3-Isoxazo                                    1-713    Pyr      CH.sub.2 CH.sub.2                                                                       3-HO-5-Isoxazo                                    1-714    Pyr      CH.sub.2 CH.sub.2                                                                       5-HO-4-Isoxazo                                    1-715    Pyr      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3-Isoxazo                             1-716    Pyr      CH.sub.2 CH.sub.2                                                                       5-Ph-3-Isoxazo                                    1-717    Pyr      CH.sub.2 CH.sub.2                                                                       4,5-diMe-3-Isoxazo                                1-718    Pyr      CH.sub.2 CH.sub.2                                                                       4-HO-5-Me-3-Isoxazo                               1-719    Pyr      CH.sub.2 CH.sub.2                                                                       2-Thiazo                                          1-720    Pyr      CH.sub.2 CH.sub.2                                                                       4-Thiazo                                          1-721    Pyr      CH.sub.2 CH.sub.2                                                                       5-Thiazo                                          1-722    Pyr      CH.sub.2 CH.sub.2                                                                       4-Me-2-Thiazo                                     1-723    Pyr      CH.sub.2 CH.sub.2                                                                       2-Me-5-Thiazo                                     1-724    Pyr      CH.sub.2 CH.sub.2                                                                       2-MeO-4-Thiazo                                    1-725    Pyr      CH.sub.2 CH.sub.2                                                                       2-MeO-5-Thiazo                                    1-726    Pyr      CH.sub.2 CH.sub.2                                                                       2-HO-5-Thiazo                                     1-727    Pyr      CH.sub.2 CH.sub.2                                                                       5-Cl-2-Thiazo                                     1-728    Pyr      CH.sub.2 CH.sub.2                                                                       2-NH.sub.2 -4-Thiazo                              1-729    Pyr      CH.sub.2 CH.sub.2                                                                       2-AcNH-4-Thiazo                                   1-730    Pyr      CH.sub.2 CH.sub.2                                                                       4,5-diMe-2-Thiazo                                 1-731    Pyr      CH.sub.2 CH.sub.2                                                                       2-HO-5-Me-4-Thiazo                                1-732    Pyr      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -2-Me-4-Thiazo                         1-733    Pyr      CH.sub.2 CH.sub.2                                                                       3-Isothiazo                                       1-734    Pyr      CH.sub.2 CH.sub.2                                                                       4-Isothiazo                                       1-735    Pyr      CH.sub.2 CH.sub.2                                                                       3-Pyrazo                                          1-736    Pyr      CH.sub.2 CH.sub.2                                                                       4-Pyrazo                                          1-737    Pyr      CH.sub.2 CH.sub.2                                                                       1-Me-3-Pyrazo                                     1-738    Pyr      CH.sub.2 CH.sub.2                                                                       1-Et-3-Pyrazo                                     1-739    Pyr      CH.sub.2 CH.sub.2                                                                       1-Me-4-Pyrazo                                     1-740    Pyr      CH.sub.2 CH.sub.2                                                                       1-Et-4-Pyrazo                                     1-741    Pyr      CH.sub.2 CH.sub.2                                                                       4-Me-3-Pyrazo                                     1-742    Pyr      CH.sub.2 CH.sub.2                                                                       5-Me-3-Pyrazo                                     1-743    Pyr      CH.sub.2 CH.sub.2                                                                       5-Me-4-Pyrazo                                     1-744    Pyr      CH.sub.2 CH.sub.2                                                                       4-MeO-3-Pyrazo                                    1-745    Pyr      CH.sub.2 CH.sub.2                                                                       4-HO-3-Pyrazo                                     1-746    Pyr      CH.sub.2 CH.sub.2                                                                       4-Cl-3-Pyrazo                                     1-747    Pyr      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3-Pyrazo                              1-748    Pyr      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -3-Pyrazo                              1-749    Pyr      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -4-Pyrazo                              1-750    Pyr      CH.sub.2 CH.sub.2                                                                       4-AcNH-3-Pyrazo                                   1-751    Pyr      CH.sub.2 CH.sub.2                                                                       5-Ph-3-Pyrazo                                     1-752    Pyr      CH.sub.2 CH.sub.2                                                                       1,5-diMe-3-Pyrazo                                 1-753    Pyr      CH.sub.2 CH.sub.2                                                                       1,4-diMe-3-Pyrazo                                 1-754    Pyr      CH.sub.2 CH.sub.2                                                                       3,5-diMe-4-Pyrazo                                 1-755    Pyr      CH.sub.2 CH.sub.2                                                                       1,5-diMe-4-Pyrazo                                 1-756    Pyr      CH.sub.2 CH.sub.2                                                                       1,3-diMe-4-Pyrazo                                 1-757    Pyr      CH.sub.2 CH.sub.2                                                                       1,3-diMe-5-Pyrazo                                 1-758    Pyr      CH.sub.2 CH.sub.2                                                                       3-Cl-5-Me-4-Pyrazo                                1-759    Pyr      CH.sub.2 CH.sub.2                                                                       3-Cl-1-Me-4-Pyrazo                                1-760    Pyr      CH.sub.2 CH.sub.2                                                                       4-Cl-5-Me-3-Pyrazo                                1-761    Pyr      CH.sub.2 CH.sub.2                                                                       4-Cl-1-Me-3-Pyrazo                                1-762    Pyr      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -5-Me-4-Pyrazo                         1-763    Pyr      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -1-Me-4-Pyrazo                         1-764    Pyr      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -1-Me-4-Pyrazo                         1-765    Pyr      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -4-Me-3-Pyrazo                         1-766    Pyr      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -1-Me-3-Pyrazo                         1-767    Pyr      CH.sub.2 CH.sub.2                                                                       5-NH.sub.2 -3-Me-4-Pyrazo                         1-768    Pyr      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -5-Me-3-Pyrazo                         1-769    Pyr      CH.sub.2 CH.sub.2                                                                       4-HO-5-Me-3-Pyrazo                                1-770    Pyr      CH.sub.2 CH.sub.2                                                                       1,3,5-triMe-4-Pyrazo                              1-771    Pyr      CH.sub.2 CH.sub.2                                                                       1,3,4-triMe-5-Pyrazo                              1-772    Pyr      CH.sub.2 CH.sub.2                                                                       4-Cl-1,3-diMe-5-Pyrazo                            1-773    Pyr      CH.sub.2 CH.sub.2                                                                       2-Imidazo                                         1-774    Pyr      CH.sub.2 CH.sub.2                                                                       4-Imidazo                                         1-775    Pyr      CH.sub.2 CH.sub.2                                                                       1-Me-4-Imidazo                                    1-776    Pyr      CH.sub.2 CH.sub.2                                                                       5-Me-4-Imidazo                                    1-777    Pyr      CH.sub.2 CH.sub.2                                                                       5-Me-2-Imidazo                                    1-778    Pyr      CH.sub.2 CH.sub.2                                                                       1-Me-2-Imidazo                                    1-779    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,3-Oxadiazo-5-yl                               1-780    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,4-Oxadiazo-5-yl                               1-781    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,5-Oxadiazo-3-yl                               1-782    Pyr      CH.sub.2 CH.sub.2                                                                       5-Me-1,2,3-Oxadiazo-4-yl                          1-783    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,3-Thiadiazo-4-yl                              1-784    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,4-Thiadiazo-3-yl                              1-785    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,5-Thiadiazo-3-yl                              1-786    Pyr      CH.sub.2 CH.sub.2                                                                       4-Me-1,2,3-Thiadiazo-5-yl                         1-787    Pyr      CH.sub.2 CH.sub.2                                                                       5-Ph-1,2,3-Thiadiaio-4-yl                         1-788    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Fur                                             1-789    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3-Fur                                             1-790    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Me-2-Fur                                        1-791    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2,4-diMe-3-Fur                                    1-792    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Thi                                             1-793    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3-Thi                                             1-794    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3-Me-2-Thi                                        1-795    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Me-3-Thi                                        1-796    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-MeO-3-Thi                                       1-797    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4,5-diMe-2-Thi                                    1-798    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Pyl                                             1-799    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3-Pyl                                             1-800    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1-Me-2-Pyl                                        1-801    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Me-2-Pyl                                        1-802    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Me-3-Pyl                                        1-803    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3,5-diMe-2-Pyl                                    1-804    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1,3-diMe-2-Pyl                                    1-805    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Oxazo                                           1-806    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       5-Oxazo                                           1-807    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Oxazo                                           1-808    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Me-4-Oxazo                                      1-809    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2,5-diMe-4-Oxazo                                  1-810    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3-Isoxazo                                         1-811    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Isoxazo                                         1-812    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       5-Me-3-Isoxazo                                    1-813    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-MeO-3-Isoxazo                                   1-814    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-HO-3-Isoxazo                                    1-815    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4,5-diMe-3-Isoxazo                                1-816    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-HO-5-Me-3-Isoxazo                               1-817    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Thiazo                                          1-818    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Thiazo                                          1-819    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       5-Thiazo                                          1-820    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Me-2-Thiazo                                     1-821    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Me-5-Thiazo                                     1-822    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-MeO-4-Thiazo                                    1-823    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4,5-diMe-2-Thiazo                                 1-824    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3-Isothiazo                                       1-825    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Isothiazo                                       1-826    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3-Pyrazo                                          1-827    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Pyrazo                                          1-828    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1-Me-3-Pyrazo                                     1-829    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1-Me-4-Pyrazo                                     1-830    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Me-3-Pyrazo                                     1-831    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       5-Me-3-Pyrazo                                     1-832    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       5-Me-4-Pyrazo                                     1-833    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-MeO-3-Pyrazo                                    1-834    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-HO-3-Pyrazo                                     1-835    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       3,5-diMe-4-Pyrazo                                 1-836    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1,3,5-triMe-4-Pyrazo                              1-837    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1,3,4-triMe-5-Pyrazo                              1-838    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       2-Imidazo                                         1-839    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       4-Imidazo                                         1-840    NMe      CH.sub.2 CH.sub.2                                                                       5-Me-4-Imidazo                                    1-841    Azi      CH.sub.2 CH.sub.2                                                                       2-Fur                                             1-842    Azi      CH.sub.2 CH.sub.2                                                                       3-Fur                                             1-843    Azi      CH.sub.2 CH.sub.2                                                                       4-Me-2-Fur                                        1-844    Azi      CH.sub.2 CH.sub.2                                                                       2-Thi                                             1-845    Azi      CH.sub.2 CH.sub.2                                                                       3-Thi                                             1-846    Azi      CH.sub.2 CH.sub.2                                                                       5-Me-2-Thi                                        1-847    Azi      CH.sub.2 CH.sub.2                                                                       2-Pyl                                             1-848    Azi      CH.sub.2 CH.sub.2                                                                       3-Pyl                                             1-849    Azi      CH.sub.2 CH.sub.2                                                                       1-Me-2-Pyl                                        1-850    Azi      CH.sub.2 CH.sub.2                                                                       4-Me-2-Pyl                                        1-851    Azi      CH.sub.2 CH.sub.2                                                                       4-Oxazo                                           1-852    Azi      CH.sub.2 CH.sub.2                                                                       5-Oxazo                                           1-853    Azi      CH.sub.2 CH.sub.2                                                                       2-Oxazo                                           1-854    Azi      CH.sub.2 CH.sub.2                                                                       3-Isoxazo                                         1-855    Azi      CH.sub.2 CH.sub.2                                                                       4-Isoxazo                                         1-856    Azi      CH.sub.2 CH.sub.2                                                                       4-HO-3-Isoxazo                                    1-857    Azi      CH.sub.2 CH.sub.2                                                                       2-Thiazo                                          1-858    Azi      CH.sub.2 CH.sub.2                                                                       4-Thiazo                                          1-859    Azi      CH.sub.2 CH.sub.2                                                                       5-Thiazo                                          1-860    Azi      CH.sub.2 CH.sub.2                                                                       2-Me-5-Thiazo                                     1-861    Azi      CH.sub.2 CH.sub.2                                                                       3-Pyrazo                                          1-862    Azi      CH.sub.2 CH.sub.2                                                                       4-Pyrazo                                          1-863    Azi      CH.sub.2 CH.sub.2                                                                       1-Me-3-Pyrazo                                     1-864    Azi      CH.sub.2 CH.sub.2                                                                       4-Me-3-Pyrazo                                     1-865    Azi      CH.sub.2 CH.sub.2                                                                       5-Me-4-Pyrazo                                     1-866    Azi      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3-Pyrazo                              1-867    Azi      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -4-Pyrazo                              1-868    Azi      CH.sub.2 CH.sub.2                                                                       3,5-diMe-4-Pyrazo                                 1-869    Azi      CH.sub.2 CH.sub.2                                                                       1,3,5-triMe-4-Pyrazo                              1-870    Azi      CH.sub.2 CH.sub.2                                                                       2-Imidazo                                         1-871    Azi      CH.sub.2 CH.sub.2                                                                       4-Imidazo                                         1-872    Azi      CH.sub.2 CH.sub.2                                                                       5-Me-4-Imidazo                                    1-873    Aze      CH.sub.2 CH.sub.2                                                                       2-Fur                                             1-874    Aze      CH.sub.2 CH.sub.2                                                                       3-Fur                                             1-875    Aze      CH.sub.2 CH.sub.2                                                                       4-Me-2-Fur                                        1-876    Aze      CH.sub.2 CH.sub.2                                                                       2-Thi                                             1-877    Aze      CH.sub.2 CH.sub.2                                                                       3-Thi                                             1-878    Aze      CH.sub.2 CH.sub.2                                                                       5-Me-2-Thi                                        1-879    Aze      CH.sub.2 CH.sub.2                                                                       2-Pyl                                             1-880    Aze      CH.sub.2 CH.sub.2                                                                       3-Pyl                                             1-881    Aze      CH.sub.2 CH.sub.2                                                                       1-Me-2-Pyl                                        1-882    Aze      CH.sub.2 CH.sub.2                                                                       4-Me-2-Pyl                                        1-883    Aze      CH.sub.2 CH.sub.2                                                                       4-Oxazo                                           1-884    Aze      CH.sub.2 CH.sub.2                                                                       5-Oxazo                                           1-885    Aze      CH.sub.2 CH.sub.2                                                                       2-Oxazo                                           1-886    Aze      CH.sub.2 CH.sub.2                                                                       3-Isoxazo                                         1-887    Aze      CH.sub.2 CH.sub.2                                                                       4-Isoxazo                                         1-888    Aze      CH.sub.2 CH.sub.2                                                                       4-HO-3-Isoxazo                                    1-889    Aze      CH.sub.2 CH.sub.2                                                                       2-Thiazo                                          1-890    Aze      CH.sub.2 CH.sub.2                                                                       4-Thiazo                                          1-891    Aze      CH.sub.2 CH.sub.2                                                                       5-Thiazo                                          1-892    Aze      CH.sub.2 CH.sub.2                                                                       2-Me-5-Thiazo                                     1-893    Aze      CH.sub.2 CH.sub.2                                                                       3-Pyrazo                                          1-894    Aze      CH.sub.2 CH.sub.2                                                                       4-Pyrazo                                          1-895    Aze      CH.sub.2 CH.sub.2                                                                       1-Me-3-Pyrazo                                     1-896    Aze      CH.sub.2 CH.sub.2                                                                       4-Me-3-Pyrazo                                     1-897    Aze      CH.sub.2 CH.sub.2                                                                       5-Me-4-Pyrazo                                     1-898    Aze      CH.sub.2 CH.sub.2                                                                       4-NH.sub.2 -3-Pyrazo                              1-899    Aze      CH.sub.2 CH.sub.2                                                                       3-NH.sub.2 -4-Pyrazo                              1-900    Aze      CH.sub.2 CH.sub.2                                                                       3,5-diMe-4-Pyrazo                                 1-901    Aze      CH.sub.2 CH.sub.2                                                                       1,3,5-triMe-4-Pyrazo                              1-902    Aze      CH.sub.2 CH.sub.2                                                                       2-Imidazo                                         1-903    Aze      CH.sub.2 CH.sub.2                                                                       4-Imidazo                                         1-904    Aze      CH.sub.2 CH.sub.2                                                                       5-Me-4-Imidazo                                    1-905    Pip      CH.sub.2 CH.sub.2                                                                       1,2,3-Triazo-4-yl                                 1-906    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-1,2,3-Triazo-4-yl                            1-907    Pip      CH.sub.2 CH.sub.2                                                                       5-Me-1,2,3-Triazo-4-yl                            1-908    Pip      CH.sub.2 CH.sub.2                                                                       1,5-diMe-1,2,3-Triazo-4-yl                        1-909    Pip      CH.sub.2 CH.sub.2                                                                       1,2,4-Triazo-5-yl                                 1-910    Pip      CH.sub.2 CH.sub.2                                                                       1-Me-1,2,5-Triazo-3-yl                            1-911    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,3-Triazo-4-yl                                 1-912    Pyr      CH.sub.2 CH.sub.2                                                                       1,2,4-Triazo-5-yl                                 1-913    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1,2,3-Triazo-4-yl                                 1-914    NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       1,2,4-Triazo-5-yl                                 1-915    Pip      CH.sub.2  1,2,3-Triazo-4-yl                                 1-916    Pip      CH.sub.2  2-Fur                                             1-917    Pip      CH.sub.2  3-Fur                                             1-918    Pip      CH.sub.2  4-Me-2-Fur                                        1-919    Pip      CH.sub.2  2,4-diMe-3-Fur                                    1-920    Pip      CH.sub.2  2-Thi                                             1-921    Pip      CH.sub.2  3-Thi                                             1-922    Pip      CH.sub.2  3-Me-2-Thi                                        1-923    Pip      CH.sub.2  2-Me-3-Thi                                        1-924    Pip      CH.sub.2  4-MeO-3-Thi                                       1-925    Pip      CH.sub.2  4,5-diMe-2-Thi                                    1-926    Pip      CH.sub.2  2-Pyl                                             1-927    Pip      CH.sub.2  3-Pyl                                             1-928    Pip      CH.sub.2  1-Me-2-Pyl                                        1-929    Pip      CH.sub.2  4-Me-2-Pyl                                        1-930    Pip      CH.sub.2  2-Me-3-Pyl                                        1-931    Pip      CH.sub.2  3,5-diMe-2-Pyl                                    1-932    Pip      CH.sub.2  1,3-diMe-2-Pyl                                    1-933    Pip      CH.sub.2  5-NH.sub.2 -1-Me-2-Pyl                            1-934    Pip      CH.sub.2  4-Oxazo                                           1-935    Pip      CH.sub.2  5-Oxazo                                           1-936    Pip      CH.sub.2  2-Oxazo                                           1-937    Pip      CH.sub.2  2-Me-4-Oxazo                                      1-938    Pip      CH.sub.2  2,5-diMe-4-Oxazo                                  1-939    Pip      CH.sub.2  3-Isoxazo                                         1-940    Pip      CH.sub.2  4-Isoxazo                                         1-941    Pip      CH.sub.2  5-Me-3-Isoxazo                                    1-942    Pip      CH.sub.2  4,5-diMe-3-Isoxazo                                1-943    Pip      CH.sub.2  2-Thiazo                                          1-944    Pip      CH.sub.2  4-Thiazo                                          1-945    Pip      CH.sub.2  5-Thiazo                                          1-946    Pip      CH.sub.2  2-Me-5-Thiazo                                     1-947    Pip      CH.sub.2  4,5-diMe-2-Thiazo                                 1-948    Pip      CH.sub.2  3-Isothiazo                                       1-949    Pip      CH.sub.2  4-Isothiazo                                       1-950    Pip      CH.sub.2  3-Pyrazo                                          1-951    Pip      CH.sub.2  4-Pyrazo                                          1-952    Pip      CH.sub.2  1-Me-3-Pyrazo                                     1-953    Pip      CH.sub.2  1-Me-4-Pyrazo                                     1-954    Pip      CH.sub.2  4-Me-3-Pyrazo                                     1-955    Pip      CH.sub.2  5-Me-3-Pyrazo                                     1-956    Pip      CH.sub.2  5-Me-4-Pyrazo                                     1-957    Pip      CH.sub.2  4-MeO-3-Pyrazo                                    1-958    Pip      CH.sub.2  4-HO-3-Pyrazo                                     1-959    Pip      CH.sub.2  4-Cl-3-Pyrazo                                     1-960    Pip      CH.sub.2  4-NH.sub.2 -3-Pyrazo                              1-961    Pip      CH.sub.2  5-NH.sub.2 -3-Pyrazo                              1-962    Pip      CH.sub.2  3-NH.sub.2 -4-Pyrazo                              1-963    Pip      CH.sub.2  5-Ph-3-Pyrazo                                     1-964    Pip      CH.sub.2  3,5-diMe-4-Pyrazo                                 1-965    Pip      CH.sub.2  3-NH.sub.2 -5-Me-4-Pyrazo                         1-966    Pip      CH.sub.2  5-NH.sub.2 -4-Me-3-Pyrazo                         1-967    Pip      CH.sub.2  5-NH.sub.2 -3-Me-3-Pyrazo                         1-968    Pip      CH.sub.2  4-NH.sub.2 -5-Me-3-Pyrazo                         1-969    Pip      CH.sub.2  1,3,5-triMe-4-Pyrazo                              1-970    Pip      CH.sub.2  1,3,4-triMe-5-Pyrazo                              1-971    Pip      CH.sub.2  2-Imidazo                                         1-972    Pip      CH.sub.2  4-Imidazo                                         1-973    Pip      CH.sub.2  5-Me-4-Imidazo                                    1-974    Pip      CH═CH NHiPr                                             1-975    Pip      CH═CH NHsBu                                             1-976    Pip      CH═CH NH(1-MeBu)                                        1-977    Pip      CH═CH NH(1,2-diMePr)                                    1-978    Pip      CH═CH NH(1-MePn)                                        1-979    Pip      CH═CH NH(1,3-diMeBu)                                    1-980    Pip      CH═CH NH(1,2-diMeBu)                                    1-981    Pip      CH═CH NH(1-MeHx)                                        1-982    Pip      CH═CH NH(1,4-diMePn)                                    1-983    Pip      CH═CH NH(1-MeHp)                                        1-984    Pip      CH═CH NH(1,5-diMeHx)                                    1-985    Pip      CH═CH NH(1-EtPr)                                        1-986    Pip      CH═CH NH(1-EtBu)                                        1-987    Pip      CH═CH NH(1-Et-2-MePr)                                   1-988    Pip      CH═CH NH(1-EtPn)                                        1-989    Pip      CH═CH NH(1-Et-3-MeBu)                                   1-990    Pip      CH═CH NH(1-EtHx)                                        1-991    Pip      CH═CH NH(1-EtHp)                                        1-992    Pip      CH═CH NH(1-PrBu)                                        1-993    Pip      CH═CH NH(1-iPrBu)                                       1-994    Pip      CH═CH NH(1-PrPn)                                        1-995    Pip      CH═CH NH(1-PrHx)                                        1-996    Pip      CH═CH NH(1-PrHp)                                        1-997    Pip      CH═CH NH(1-BuPn)                                        1-998    Pip      CH═CH NH(1-PnHx)                                        1-999    Pip      CH═CH NH(1-HxHp)                                        1-1000   Pip      CH═CH NH(1-PhEt)                                        1-1001   Pip      CH═CH NH(1-NaPhEt)                                      1-1002   Pip      CH═CH NH(1-PhPr)                                        1-1003   Pip      CH═CH NH(1-PhBu)                                        1-1004   Pip      CH═CH NHCHPh.sub.2                                      1-1005   Pip      CH═CH NHCHPh(4-MePh)                                    1-1006   Pip      CH═CH NHCHPh(4-MeOPh)                                   1-1007   Pip      CH═CH NHCHPh(4-FPh)                                     1-1008   Pip      CH═CH NHCHPh(4-ClPh)                                    1-1009   Pip      CH═CH NH(1-Me-2-PhEt)                                   1-1010   Pip      CH═CH NH(1-Me-3-PhPr)                                   1-1011   Pip      CH═CH NH(1-Et-2-PhEt)                                   1-1012   Pip      CH═CH NH[1-Me-2-(4-MePh)Et]                             1-1013   Pip      CH═CH NH[1-Me-2-(4-MeOPh)Et]                            1-1014   Pip      CH═CH NH[1-Me-2-(4-FPh)Et]                              1-1015   Pip      CH═CH NH[1-Me-2-(4-ClPh)Et]                             1-1016   Pip      CH═CH NH(1,2-diPhEt)                                    1-1017   Pip      CH═CH NH(1-Bz-2-PhEt)                                   1-1018   Pip      CH═CH NHcPr                                             1-1019   Pip      CH═CH NHcBu                                             1-1020   Pip      CH═CH NHcPn                                             1-1021   Pip      CH═CH NHcHx                                             1-1022   Pip      CH═CH NHcHp                                             1-1023   Pip      CH═CH NHcOc                                             1-1024   Pyr      CH═CH NHiPr                                             1-1025   Pyr      CH═CH NHsBu                                             1-1026   Pyr      CH═CH NH(1-MeBu)                                        1-1027   Pyr      CH═CH NH(1-MePn)                                        1-1028   Pyr      CH═CH NH(1-MeHx)                                        1-1029   Pyr      CH═CH NH(1-MeHp)                                        1-1030   Pyr      CH═CH NH(1-EtPr)                                        1-1031   Pyr      CH═CH NH(1-EtBu)                                        1-1032   Pyr      CH═CH NH(1-EtPn)                                        1-1033   Pyr      CH═CH NH(1-PrBu)                                        1-1034   Pyr      CH═CH NH(1-BuPn)                                        1-1035   Pyr      CH═CH NH(1-PhEt)                                        1-1036   Pyr      CH═CH NH(1-NaPhEt)                                      1-1037   Pyr      CH═CH NH(1-PhPr)                                        1-1038   Pyr      CH═CH NHCHPh.sub.2                                      1-1039   Pyr      CH═CH NHCHPh(4-MePh)                                    1-1040   Pyr      CH═CH NHCHPh(4-MeoPh)                                   1-1041   Pyr      CH═CH NHCHPh(4-FPh)                                     1-1042   Pyr      CH═CH NHCHPh(4-ClPh)                                    1-1043   Pyr      CH═CH NH(1-Me-2-PhEt)                                   1-1044   Pyr      CH═CH NH[1-Me-2-(4-MePh)Et]                             1-1045   Pyr      CH═CH NH[1-Me-2-(4-MeOPh)Et]                            1-1046   Pyr      CH═CH NH[1-Me-2-(4-FPh)Et]                              1-1047   Pyr      CH═CH NH(1-Bz-2-PhEt)                                   1-1048   Pyr      CH═CH NHcPr                                             1-1049   Pyr      CH═CH NHcBu                                             1-1050   Pyr      CH═CH NHcPn                                             1-1051   Pyr      CH═CH NHcHx                                             1-1052   Pyr      CH═CH NHcHp                                             1-1053   Pyr      CH═CH NHcOc                                             1-1054   NMe.sub.2                                                                              CH═CH NHiPr                                             1-1055   NMe.sub.2                                                                              CH═CH NHsBu                                             1-1056   NMe.sub.2                                                                              CH═CH NH(1-MeBu)                                        1-1057   NMe.sub.2                                                                              CH═CH NH(1-MePn)                                        1-1058   NMe.sub.2                                                                              CH═CH NH(1-MeHx)                                        1-1059   NMe.sub.2                                                                              CH═CH NH(1-MeHp)                                        1-1060   NMe.sub.2                                                                              CH═CH NH(1-EtPr)                                        1-1061   NMe.sub.2                                                                              CH═CH NH(1-EtBu)                                        1-1062   NMe.sub.2                                                                              CH═CH NH(1-EtPn)                                        1-1063   NMe.sub.2                                                                              CH═CH NH(1-PrBu)                                        1-1064   NMe.sub.2                                                                              CH═CH NH(1-BuPn)                                        1-1065   NMe.sub.2                                                                              CH═CH NH(1-PhEt)                                        1-1066   NMe.sub.2                                                                              CH═CH NH(1-NaPhEt)                                      1-1067   NMe.sub.2                                                                              CH═CH NH(1-PhPr)                                        1-1068   NMe.sub.2                                                                              CH═CH NHCHPh.sub.2                                      1-1069   NMe.sub.2                                                                              CH═CH NHCHPh(4-MePh)                                    1-1070   NMe.sub.2                                                                              CH═CH NHCHPh(4-MeOPh)                                   1-1071   NMe.sub.2                                                                              CH═CH NHCHPh(4-FPh)                                     1-1072   NMe.sub.2                                                                              CH═CH NHCHPh(4-ClPh)                                    1-1073   NMe.sub.2                                                                              CH═CH NH(1-Me-2-PhEt)                                   1-1074   NMe.sub.2                                                                              CH═CH NH[1-Me-2-(4-MePh)Et]                             1-1075   NMe.sub.2                                                                              CH═CH NH[1-Me-2-(4-MeOPh)Et]                            1-1076   NMe.sub.2                                                                              CH═CH NH[1-Me-2-(4-FPh)Et]                              1-1077   NMe.sub.2                                                                              CH═CH NH(1-Bz-2-PhEt)                                   1-1078   NMe.sub.2                                                                              CH═CH NHcPr                                             1-1079   NMe.sub.2                                                                              CH═CH NHcBu                                             1-1080   NMe.sub.2                                                                              CH═CH NHcPn                                             1-1081   NMe.sub.2                                                                              CH═CH NHcHx                                             1-1082   NMe.sub.2                                                                              CH═CH NHcHp                                             1-1083   NMe.sub.2                                                                              CH═CH NHcOc                                             1-1084   Aze      CH═CH NHiPr                                             1-1085   Aze      CH═CH NHsBu                                             1-1086   Aze      CH═CH NH(1-MeBu)                                        1-1087   Aze      CH═CH NH(1-MePn)                                        1-1088   Aze      CH═CH NH(1-MeHx)                                        1-1089   Aze      CH═CH NH(1-MeHp)                                        1-1090   Aze      CH═CH NH(1-EtPr)                                        1-1091   Aze      CH═CH NH(1-EtBu)                                        1-1092   Aze      CH═CH NH(1-EtPn)                                        1-1093   Aze      CH═CH NH(1,2-diMePr)                                    1-1094   Aze      CH═CH NH(1-PhEt)                                        1-1095   Aze      CH═CH NHCHPh.sub.2                                      1-1096   Aze      CH═CH NH(1-Me-2-PhEt)                                   1-1097   Aze      CH═CH NH(1,2-diPhEt)                                    1-1098   Aze      CH═CH NHcPr                                             1-1099   Aze      CH═CH NHcBu                                             1-1100   Aze      CH═CH NHcPn                                             1-1101   Aze      CH═CH NHcHx                                             1-1102   Aze      CH═CH NHcHp                                             1-1103   Aze      CH═CH NHcOc                                             1-1104   Azi      CH═CH NHiPr                                             1-1105   Azi      CH═CH NHsBu                                             1-1106   Azi      CH═CH NH(1-MeBu)                                        1-1107   Azi      CH═CH NH(1-MePn)                                        1-1108   Azi      CH═CH NH(1-MeHx)                                        1-1109   Azi      CH═CH NH(1-MeHp)                                        1-1110   Azi      CH═CH NH(1-EtPr)                                        1-1111   Azi      CH═CH NH(1-EtBu)                                        1-1112   Azi      CH═CH NH(1-EtPn)                                        1-1113   Azi      CH═CH NH(1,2-diMePr)                                    1-1114   Azi      CH═CH NH(1-PhEt)                                        1-1115   Azi      CH═CH NHCHPh 2                                          1-1116   Azi      CH═CH NH(1-Me-2-PhEt)                                   1-1117   Azi      CH═CH NH(1,2-diPhEt)                                    1-1118   Azi      CH═CH NHcPr                                             1-1119   Azi      CH═CH NHcBu                                             1-1120   Azi      CH═CH NHcPn                                             1-1121   Azi      CH═CH NHcHx                                             1-1122   Azi      CH═CH NHcHp                                             1-1123   Azi      CH═CH NHcOc                                             1-1124   Pip      CH.sub.2 CH.sub.2                                                                       NHiPr                                             1-1125   Pip      CH.sub.2 CH.sub.2                                                                       NHsBu                                             1-1126   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-MeBu)                                        1-1127   Pip      CH.sub.2 CH.sub.2                                                                       NH(1,2-diMePr)                                    1-1128   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-MePn)                                        1-1129   Pip      CH.sub.2 CH.sub.2                                                                       NH(1,3-diMeBu)                                    1-1130   Pip      CH.sub.2 CH.sub.2                                                                       NH(1,2-diMeBu)                                    1-1131   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-MeHx)                                        1-1132   Pip      CH.sub.2 CH.sub.2                                                                       NH(1,4-diMePn)                                    1-1133   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-MeHp)                                        1-1134   Pip      CH.sub.2 CH.sub.2                                                                       NH(1,5-diMeHx)                                    1-1135   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-EtPr)                                        1-1136   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-EtBu)                                        1-1137   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-Et-2-MePr)                                   1-1138   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-EtPn)                                        1-1139   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-Et-3-MeBu)                                   1-1140   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-EtHx)                                        1-1141   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-EtHp)                                        1-1142   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PrBu)                                        1-1143   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-iPrBu)                                       1-1144   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PrPn)                                        1-1145   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PrHx)                                        1-1146   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PrHp)                                        1-1147   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-BuPn)                                        1-1148   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PnHx)                                        1-1149   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-HxHp)                                        1-1150   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PhEt)                                        1-1151   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-NaPhEt)                                      1-1152   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PhPr)                                        1-1153   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-PhBu)                                        1-1154   Pip      CH.sub.2 CH.sub.2                                                                       NHCHPh.sub.2                                      1-1155   Pip      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-MePh)                                    1-1156   Pip      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-MeOPh)                                   1-1157   Pip      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-FPh)                                     1-1158   Pip      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-ClPh)                                    1-1159   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-Me-2-PhEt)                                   1-1160   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-Me-3-PhPr)                                   1-1161   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-Et-2-PhEt)                                   1-1162   Pip      CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-MePh)Et]                             1-1163   Pip      CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-MeOPh)Et]                            1-1164   Pip      CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-FPh)Et]                              1-1165   Pip      CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-ClPh)Et]                             1-1166   Pip      CH.sub.2 CH.sub.2                                                                       NH(1,2-diPhEt)                                    1-1167   Pip      CH.sub.2 CH.sub.2                                                                       NH(1-Bz-2-PhEt)                                   1-1168   Pip      CH.sub.2 CH.sub.2                                                                       NHcPr                                             1-1169   Pip      CH.sub.2 CH.sub.2                                                                       NHcBu                                             1-1170   Pip      CH.sub.2 CH.sub.2                                                                       NHcPn                                             1-1171   Pip      CH.sub.2 CH.sub.2                                                                       NHcHx                                             1-1172   Pip      CH.sub.2 CH.sub.2                                                                       NHcHp                                             1-1173   Pip      CH.sub.2 CH.sub.2                                                                       NHcOc                                             1-1174   Pyr      CH.sub.2 CH.sub.2                                                                       NHiPr                                             1-1175   Pyr      CH.sub.2 CH.sub.2                                                                       NHsBu                                             1-1176   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-MeBu)                                        1-1177   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-MePn)                                        1-1178   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-MeHx)                                        1-1179   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-MeHp)                                        1-1180   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-EtPr)                                        1-1181   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-EtBu)                                        1-1182   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-EtPn)                                        1-1183   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-PrBu)                                        1-1184   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-BuPn)                                        1-1185   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-PhEt)                                        1-1186   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-NaPhEt)                                      1-1187   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-PhPr)                                        1-1188   Pyr      CH.sub.2 CH.sub.2                                                                       NHCHPh.sub.2                                      1-1189   Pyr      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-MePh)                                    1-1190   Pyr      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-MeOPh)                                   1-1191   Pyr      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-FPh)                                     1-1192   Pyr      CH.sub.2 CH.sub.2                                                                       NHCHPh(4-ClPh)                                    1-1193   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-Me-2-PhEt)                                   1-1194   Pyr      CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-MePh)Et]                             1-1195   Pyr      CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-MeOPh)Et]                            1-1196   Pyr      CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-FPh)Et]                              1-1197   Pyr      CH.sub.2 CH.sub.2                                                                       NH(1-Bz-2-PhEt)                                   1-1198   Pyr      CH.sub.2 CH.sub.2                                                                       NHcPr                                             1-1199   Pyr      CH.sub.2 CH.sub.2                                                                       NHcBu                                             1-1200   Pyr      CH.sub.2 CH.sub.2                                                                       NHcPn                                             1-1201   Pyr      CH.sub.2 CH.sub.2                                                                       NHcHx                                             1-1202   Pyr      CH.sub.2 CH.sub.2                                                                       NHcHp                                             1-1203   Pyr      CH.sub.2 CH.sub.2                                                                       NHcOc                                             1-1204   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHiPr                                             1-1205   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHsBu                                             1-1206   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-MeBu)                                        1-1207   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-MePn)                                        1-1208   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-MeHx)                                        1-1209   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-MeHp)                                        1-1210   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-EtPr)                                        1-1211   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-EtBu)                                        1-1212   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-EtPn)                                        1-1213   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-PrBu)                                        1-1214   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-BuPn)                                        1-1215   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-PhEt)                                        1-1216   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-NaPhEt)                                      1-1217   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-PhPr)                                        1-1218   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHCHPh.sub.2                                      1-1219   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHCHPh(4-MePh)                                    1-1220   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHCHPh(4-MeOPh)                                   1-1221   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHCHPh(4-FPh)                                     1-1222   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHCHPh(4-ClPh)                                    1-1223   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-Me-2-PhEt)                                   1-1224   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-MePh)Et]                             1-1225   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-MeOPh)Et]                            1-1226   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH[1-Me-2-(4-FPh)Et]                              1-1227   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NH(1-Bz-2-PhEt)                                   1-1228   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHcPr                                             1-1229   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHcBu                                             1-1230   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHcPn                                             1-1231   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHcHx                                             1-1232   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHcHp                                             1-1233   NMe.sub.2                                                                              CH.sub.2 CH.sub.2                                                                       NHcOc                                             1-1234   Aze      CH.sub.2 CH.sub.2                                                                       NHiPr                                             1-1235   Aze      CH.sub.2 CH.sub.2                                                                       NHsBu                                             1-1236   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-MeBu)                                        1-1237   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-MePn)                                        1-1238   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-MeHx)                                        1-1239   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-MeHp)                                        1-1240   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-EtPr)                                        1-1241   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-EtBu)                                        1-1242   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-EtPn)                                        1-1243   Aze      CH.sub.2 CH.sub.2                                                                       NH(1,2-diMePr)                                    1-1244   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-PhEt)                                        1-1245   Aze      CH.sub.2 CH.sub.2                                                                       NHCHPh.sub.2                                      1-1246   Aze      CH.sub.2 CH.sub.2                                                                       NH(1-Me-2-PhEt)                                   1-1247   Aze      CH.sub.2 CH.sub.2                                                                       NH(1,2-diPhEt)                                    1-1248   Aze      CH.sub.2 CH.sub.2                                                                       NHcPr                                             1-1249   Aze      CH.sub.2 CH.sub.2                                                                       NHcBu                                             1-1250   Aze      CH.sub.2 CH.sub.2                                                                       NHcPn                                             1-1251   Aze      CH.sub.2 CH.sub.2                                                                       NHcHx                                             1-1252   Aze      CH.sub.2 CH.sub.2                                                                       NHcHp                                             1-1253   Aze      CH.sub.2 CH.sub.2                                                                       NHcOc                                             1-1254   Azi      CH.sub.2 CH.sub.2                                                                       NHiPr                                             1-1255   Azi      CH.sub.2 CH.sub.2                                                                       NHsBu                                             1-1256   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-MeBu)                                        1-1257   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-MePn)                                        1-1258   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-MeHx)                                        1-1259   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-MeHp)                                        1-1260   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-EtPr)                                        1-1261   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-EtBu)                                        1-1262   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-EtPn)                                        1-1263   Azi      CH.sub.2 CH.sub.2                                                                       NH(1,2-diMePr)                                    1-1264   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-PhEt)                                        1-1265   Azi      CH.sub.2 CH.sub.2                                                                       NHCHPh.sub.2                                      1-1266   Azi      CH.sub.2 CH.sub.2                                                                       NH(1-Me-2-PhEt)                                   1-1267   Azi      CH.sub.2 CH.sub.2                                                                       NH(1,2-diPhEt)                                    1-1268   Azi      CH.sub.2 CH.sub.2                                                                       NHcPr                                             1-1269   Azi      CH.sub.2 CH.sub.2                                                                       NHcBu                                             1-1270   Azi      CH.sub.2 CH.sub.2                                                                       NHcPn                                             1-1271   Azi      CH.sub.2 CH.sub.2                                                                       NHcHx                                             1-1272   Azi      CH.sub.2 CH.sub.2                                                                       NHcHp                                             1-1273   Azi      CH.sub.2 CH.sub.2                                                                       NHcOc                                             1-1274   Pip      CH.sub.2  NHiPr                                             1-1275   Pip      CH.sub.2  NHsBu                                             1-1276   Pip      CH.sub.2  NH(1-MeBu)                                        1-1277   Pip      CH.sub.2  NH(1,2-diMePr)                                    1-1278   Pip      CH.sub.2  NH(1-MePn)                                        1-1279   Pip      CH.sub.2  NH(1,3-diMeBu)                                    1-1280   Pip      CH.sub.2  NH(1,2-diMeBu)                                    1-1281   Pip      CH.sub.2  NH(1-MeHx)                                        1-1282   Pip      CH.sub.2  NH(1,4-diMePn)                                    1-1283   Pip      CH.sub.2  NH(1-MeHp)                                        1-1284   Pip      CH.sub.2  NH(1,5-diMeHx)                                    1-1285   Pip      CH.sub.2  NH(1-EtPr)                                        1-1286   Pip      CH.sub.2  NH(1-EtBu)                                        1-1287   Pip      CH.sub.2  NH.(1-Et-2-MePr)                                  1-1288   Pip      CH.sub.2  NH(1-EtPn)                                        1-1289   Pip      CH.sub.2  NH(1-Et-3-MeBu)                                   1-1290   Pip      CH.sub.2  NH(1-EtHx)                                        1-1291   Pip      CH.sub.2  NH(1-EtHp)                                        1-1292   Pip      CH.sub.2  NH(1-PrBu)                                        1-1293   Pip      CH.sub.2  NH(1-iPrBu)                                       1-1294   Pip      CH.sub.2  NH(1-PrPn)                                        1-1295   Pip      CH.sub.2  NH(1-PrHx)                                        1-1296   Pip      CH.sub.2  NH(1-PrHp)                                        1-1297   Pip      CH.sub.2  NH(1-BuPn)                                        1-1298   Pip      CH.sub.2  NH(1-PnHx)                                        1-1299   Pip      CH.sub.2  NH(1-HxHp)                                        1-1300   Pip      CH.sub.2  NH(1-PhEt)                                        1-1301   Pip      CH.sub.2  NH(1-NaPhEt)                                      1-1302   Pip      CH.sub.2  NH(1-PhPr)                                        1-1303   Pip      CH.sub.2  NH(1-PhBu)                                        1-1304   Pip      CH.sub.2  NHCHPh.sub.2                                      1-1305   Pip      CH.sub.2  NHCHPh(4-MePh)                                    1-1306   Pip      CH.sub.2  NHCHPh(4-MeOPh)                                   1-1307   Pip      CH.sub.2  NHCHPh(4-FPh)                                     1-1308   Pip      CH.sub.2  NHCHPh(4-ClPh)                                    1-1309   Pip      CH.sub.2  NH(1-Me-2-PhEt)                                   1-1310   Pip      CH.sub.2  NH(1-Me-3-PhPr)                                   1-1311   Pip      CH.sub.2  NH(1-Et-2-PhEt)                                   1-1312   Pip      CH.sub.2  NH[1-Me-2-(4-MePh)Et]                             1-1313   Pip      CH.sub.2  NH[1-Me-2-(4-MeOPh)Et]                            1-1314   Pip      CH.sub.2  NH[1-Me-2-(4-FPh)Et]                              1-1315   Pip      CH.sub.2  NH[1-Me-2-(4-ClPh)Et]                             1-1316   Pip      CH.sub.2  NH(1,2-diPhEt)                                    1-1317   Pip      CH.sub.2  NH(1-Bz-2-PhEt)                                   1-1318   Pip      CH.sub.2  NHcPr                                             1-1319   Pip      CH.sub.2  NHcBu                                             1-1320   Pip      CH.sub.2  NHcPn                                             1-1321   Pip      CH.sub.2  NHcHx                                             1-1322   Pip      CH.sub.2  NHcHp                                             1-1323   Pip      CH.sub.2  NHcOc                                             1-1324   Pip      (CH.sub.2).sub.3                                                                        NHiPr                                             1-1325   Pip      (CH.sub.2).sub.3                                                                        NHsBu                                             1-1326   Pip      (CH.sub.2).sub.3                                                                        NH(1-MeBu)                                        1-1327   Pip      (CH.sub.2).sub.3                                                                        NH(1-MePn)                                        1-1328   Pip      (CH.sub.2).sub.3                                                                        NH(1-MeHx)                                        1-1329   Pip      (CH.sub.2).sub.3                                                                        NH(1-MeHp)                                        1-1330   Pip      (CH.sub.2).sub.3                                                                        NH(1-EtPr)                                        1-1331   Pip      (CH.sub.2).sub.3                                                                        NH(1-EtBu)                                        1-1332   Pip      (CH.sub.2).sub.3                                                                        NH(1-EtPn)                                        1-1333   Pip      (CH.sub.2).sub.3                                                                        NH(1-PrBu)                                        1-1334   Pip      (CH.sub.2).sub.3                                                                        NH(1-BuPn)                                        1-1335   Pip      (CH.sub.2).sub.3                                                                        NH(1-PhEt)                                        1-1336   Pip      (CH.sub.2).sub.3                                                                        NH(1-NaPhEt)                                      1-1337   Pip      (CH.sub.2).sub.3                                                                        NH(1-PhPr)                                        1-1338   Pip      (CH.sub.2).sub.3                                                                        NHCHPh.sub.2                                      1-1339   Pip      (CH.sub.2).sub.3                                                                        NHCHPh(4-MePh)                                    1-1340   Pip      (CH.sub.2).sub.3                                                                        NHCHPh(4-MeOPh)                                   1-1341   Pip      (CH.sub.2).sub.3                                                                        NHCHPh(4-FPh)                                     1-1342   Pip      (CH.sub.2).sub.3                                                                        NHCHPh(4-ClPh)                                    1-1343   Pip      (CH.sub.2).sub.3                                                                        NH(1-Me-2-PhEt)                                   1-1344   Pip      (CH.sub.2).sub.3                                                                        NH[1-Me-2-(4-MePh)Et]                             1-1345   Pip      (CH.sub.2).sub.3                                                                        NH[1-Me-2-(4-MeOPh)Et]                            1-1346   Pip      (CH.sub.2).sub.3                                                                        NH[1-Me-2-(4-FPh)Et]                              1-1347   Pip      (CH.sub.2).sub.3                                                                        NH(1-Bz-2-PhEt)                                   1-1348   Pip      (CH.sub.2).sub.3                                                                        NHcPr                                             1-1349   Pip      (CH.sub.2).sub.3                                                                        NHcBu                                             1-1350   Pip      (CH.sub.2).sub.3                                                                        NHcPn                                             1-1351   Pip      (CH.sub.2).sub.3                                                                        NHcHx                                             1-1352   Pip      (CH.sub.2).sub.3                                                                        NHcHp                                             1-1353   Pip      (CH.sub.2).sub.3                                                                        NHcOc                                             ______________________________________                                    

                                      TABLE 2                                     __________________________________________________________________________    Cpd.                                                                          No. R.sup.1                                                                           A    B        m R.sup.5                                               __________________________________________________________________________    2-1 Pip CH═CH                                                                          CH.sub.2 0 CH.sub.2 OH                                           2-2 Pip CH═CH                                                                          CH.sub.2 0 2-HOEt                                                2-3 Pip CH═CH                                                                          CH.sub.2 0 2-FoOEt                                               2-4 Pip CH═CH                                                                          CH.sub.2 0 2-AcOEt                                               2-5 Pip CH═CH                                                                          CH.sub.2 0 2-PrnOEt                                              2-6 Pip CH═CH                                                                          CH.sub.2 0 2-ByrOEt                                              2-7 Pip CH═CH                                                                          CH.sub.2 0 2-iByrOEt                                             2-8 Pip CH═CH                                                                          CH.sub.2 0 2-ValOEt                                              2-9 Pip CH═CH                                                                          CH.sub.2 0 2-iValOEt                                             2-10                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(PhAcO)Et                                           2-11                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(HOOC.AcO)Et                                        2-12                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-HOOC.Prno)Et                                     2-13                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-14                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-Etc.PrnO)Et                                      2-15                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-Prc.PrnO)Et                                      2-16                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-Phc.PrnO)Et                                      2-17                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-[3-(4-MePhcO)PrnO]Et                                2-18                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-PhPrnO)Et                                        2-19                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-PhPrnO)Et                                        2-20                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-BozOEt                                              2-21                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(4-MeBozO)Et                                        2-22                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(4-MeOBozO)Et                                       2-23                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(4-FBozO)Et                                         2-24                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(4-ClBozO)Et                                        2-25                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(cPrCOO)Et                                          2-26                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(cBuCOO)Et                                          2-27                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(cPnCOO)Et                                          2-28                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Et                                          2-29                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-HOPr                                                2-30                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-FoOPr                                               2-31                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-AcOPr                                               2-32                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-PrnOPr                                              2-33                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-HOOC.PrnO)Pr                                     2-34                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-Mec.PrnO)Pr                                      2-35                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-Etc.PrnO)Pr                                      2-36                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-Phc.PrnO)Et                                      2-37                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-[3-(4-MePhcO)PrnO]Et                                2-38                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(PhAcO)Pr                                           2-39                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-BozOPr                                              2-40                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(cPnCOO)Pr                                          2-41                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Pr                                          2-42                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-HOPr                                                2-43                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-FoOPr                                               2-44                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-AcOPr                                               2-45                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-PrnOPr                                              2-46                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-(3-HOOC.PrnO)Pr                                     2-47                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-(3-Mec.PrnO)Pr                                      2-48                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-(3-Etc.PrnO)Pr                                      2-49                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-BozOPr                                              2-50                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-(cPnCOO)Pr                                          2-51                                                                              Pip CH═CH                                                                          CH.sub.2 0 3-(cHxCOO)Pr                                          2-52                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-HOBu                                                2-53                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-AcOBu                                               2-54                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(3-HOOC.PrnO)Bu                                     2-55                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-BozOBu                                              2-56                                                                              Pip CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Bu                                          2-57                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-58                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-FoOEt                                               2-59                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-60                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-PrnOEt                                              2-61                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-ValOEt                                              2-62                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(PhAcO)Et                                           2-63                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Et                                     2-64                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.Prno)Et                                      2-65                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-Etc.PrnO)Et                                      2-66                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-PhPrnO)Et                                        2-67                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-BozOEt                                              2-68                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(4-MeBozO)Et                                        2-69                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(4-FBozO)Et                                         2-70                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(4-ClBozO)Et                                        2-71                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cPrCOO)Et                                          2-72                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cBuCOO)Et                                          2-73                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Et                                          2-74                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Et                                          2-75                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOPr                                                2-76                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-FoOPr                                               2-77                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOPr                                               2-78                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-PrnOPr                                              2-79                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Pr                                     2-80                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.Prno)Pr                                      2-81                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-BozOPr                                              2-82                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Pr                                          2-83                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Pr                                          2-84                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-85                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-86                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-PrnOPr                                              2-87                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-(3-HOOC.PrnO)Pr                                     2-88                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-BozOPr                                              2-89                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-(cPnCOO)Pr                                          2-90                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-(cHxCOO)Pr                                          2-91                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOBu                                                2-92                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOBu                                               2-93                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Bu                                     2-94                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-BozOBu                                              2-95                                                                              Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Bu                                          2-96                                                                              Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-97                                                                              Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-FoOEt                                               2-98                                                                              Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-99                                                                              Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-100                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-ByrOEt                                              2-101                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-iByrOEt                                             2-102                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-ValOEt                                              2-103                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-104                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-Mec.PrnO)Et                                      2-105                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-Etc.PrnO)Et                                      2-106                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(PhAcO)Et                                           2-107                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-108                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(4-MeBozO)Et                                        2-109                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(4-MeOBozO)Et                                       2-110                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(4-FBozO)Et                                         2-111                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(4-ClBozO)Et                                        2-112                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cPrCOO)Et                                          2-113                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cBuCOO)Et                                          2-114                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Et                                          2-115                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-116                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOPr                                                2-117                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOPr                                               2-118                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-PrnOPr                                              2-119                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-120                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-Etc.PrnO)Pr                                      2-121                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-BozOPr                                              2-122                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Pr                                          2-123                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-124                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-125                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-126                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-(3-Mec.PrnO)Pr                                      2-127                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-BozOPr                                              2-128                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-(cHxCOO)Pr                                          2-129                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-130                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-131                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-132                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-BozOBu                                              2-133                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Bu                                          2-134                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-135                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-FoOEt                                               2-136                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-137                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-PrnOEt                                              2-138                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Et                                     2-139                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(3-Mec.PrnO)Et                                      2-140                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-BozOEt                                              2-141                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Et                                          2-142                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOPr                                                2-143                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOPr                                               2-144                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-145                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-BozOPr                                              2-146                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Pr                                          2-147                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-148                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-149                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-150                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-BozOPr                                              2-151                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-(cHxCOO)Pr                                          2-152                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOBu                                                2-153                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-154                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-155                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Bu                                          2-156                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-157                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-158                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(3-HOOC.PrnO)Et                                     2-159                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-BozOEt                                              2-160                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Et                                          2-161                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-162                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-163                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-BozOPr                                              2-164                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Pr                                          2-165                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-HOPr                                                2-166                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-167                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-(3-HOOC.PrnO)Pr                                     2-168                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-BozOPr                                              2-169                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-(cHxCOO)Pr                                          2-170                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOBu                                                2-171                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-172                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(3-Etc.PrnO)Bu                                      2-173                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Bu                                          2-174                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-175                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-176                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Et                                     2-177                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-BozOEt                                              2-178                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Et                                          2-179                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-HOPr                                                2-180                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOPr                                               2-181                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-182                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-BozOPr                                              2-183                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Pr                                          2-184                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-185                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-186                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-187                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-BozOPr                                              2-188                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-(cHxCOO)Pr                                          2-189                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-HOBu                                                2-190                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOBu                                               2-191                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-192                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Bu                                          2-193                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-194                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-195                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Et                                     2-196                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Et                                          2-197                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-HOPr                                                2-198                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOPr                                               2-199                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-200                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Pr                                          2-201                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-202                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-203                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-204                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-(cHxCOO)Pr                                          2-205                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-HOBu                                                2-206                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOBu                                               2-207                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-208                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Bu                                          2-209                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-HOEt                                                2-210                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-FoOEt                                               2-211                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-AcOEt                                               2-212                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-PrnOEt                                              2-213                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-(3-HOOC.PrnO)Et                                     2-214                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-215                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-(3-Etc.PrnO)Et                                      2-216                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-BozOEt                                              2-217                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-(cPnCOO)Et                                          2-218                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Et                                          2-219                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-HOPr                                                2-220                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-AcOPr                                               2-221                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-(3-HOOC.PrnO)Pr                                     2-222                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-BozOPr                                              2-223                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Pr                                          2-224                                                                             Pyr CH═CH                                                                          CH.sub.2 0 3-HOPr                                                2-225                                                                             Pyr CH═CH                                                                          CH.sub.2 0 3-FoOPr                                               2-226                                                                             Pyr CH═CH                                                                          CH.sub.2 0 3-AcOPr                                               2-227                                                                             Pyr CH═CH                                                                          CH.sub.2 0 3-(3-HOOC.PrnO)Pr                                     2-228                                                                             Pyr CH═CH                                                                          CH.sub.2 0 3-(3-Mec.PrnO)Pr                                      2-229                                                                             Pyr CH═CH                                                                          CH.sub.2 0 3-BozOPr                                              2-230                                                                             Pyr CH═CH                                                                          CH.sub.2 0 3-(cHxCOO)Pr                                          2-231                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-HOBu                                                2-232                                                                             Pyr CH═CH                                                                          CH.sub.2 0 2-AcOBu                                               2-233                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-234                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-235                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Et                                     2-236                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.PrnO)Et                                      2-237                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-BozOEt                                              2-238                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Et                                          2-239                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Et                                          2-240                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOPr                                                2-241                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOPr                                               2-242                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Pr                                     2-243                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Pr                                          2-244                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-245                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-246                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-(cHxCOO)Pr                                          2-247                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOBu                                                2-248                                                                             Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOBu                                               2-249                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-250                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-251                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-252                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-253                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-254                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Et                                          2-255                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-256                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOPr                                                2-257                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOPr                                               2-258                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-BozOPr                                              2-259                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-260                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-261                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-262                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-263                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-264                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-265                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-266                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Et                                     2-267                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Et                                          2-268                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOPr                                                2-269                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOPr                                               2-270                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-271                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-272                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOBu                                                2-273                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-274                                                                             Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-275                                                                             Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-276                                                                             Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-277                                                                             Pye CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-278                                                                             Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-HOPr                                                2-279                                                                             Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-280                                                                             Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOBu                                                2-281                                                                             Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-282                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-283                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-284                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-HOPr                                                2-285                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOPr                                               2-286                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Pr                                          2-287                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-288                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-289                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOBu                                               2-290                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-291                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-292                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-HOPr                                                2-293                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOPr                                               2-294                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-295                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-296                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOBu                                               2-297                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-HOEt                                                2-298                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-AcOEt                                               2-299                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-PrnOEt                                              2-300                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-(3-HOOC.PrnO)Et                                     2-301                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-302                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-BozOEt                                              2-303                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Et                                          2-304                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-HOPr                                                2-305                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Pr                                          2-306                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-HOPr                                                2-307                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-AcOPr                                               2-308                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-HOBu                                                2-309                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-AcOBu                                               2-310                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-311                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-312                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-313                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-314                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-315                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-316                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-317                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-318                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-319                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-320                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Pr                                          2-321                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Pr                                          2-322                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-323                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-324                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-325                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-326                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-327                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-328                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-329                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-330                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-331                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-332                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-333                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-334                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-335                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-336                                                                             NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-337                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-338                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-339                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-340                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-341                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-342                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-343                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-344                                                                             NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-345                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-HOEt                                                2-346                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-AcOEt                                               2-347                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-PrnOEt                                              2-348                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-(3-HOOC.PrnO)Et                                     2-349                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-BozOEt                                              2-350                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-(cHxCOO)Et                                          2-351                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-HOPr                                                2-352                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-AcOPr                                               2-353                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-(3-HOOC.PrnO)Pr                                     2-354                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-BozOPr                                              2-355                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-(cHxCOO)Pr                                          2-356                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 2-AcOBu                                               2-357                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-358                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-359                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-360                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-BozOPr                                              2-361                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-AcOBu                                               2-362                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-363                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-364                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-365                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-366                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-367                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-368                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-369                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-370                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-371                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-372                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-373                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-374                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-375                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-376                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-HOPr                                                2-377                                                                             NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-378                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-379                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-380                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-381                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-382                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 2-AcOBu                                               2-383                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-384                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-385                                                                             NEt.sub.2                                                                         CH═CH                                                                          (HC2).sub.6                                                                            0 3-HOPr                                                2-386                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-387                                                                             NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 2-AcOBu                                               2-388                                                                             Azi CH═CH                                                                          CH.sub.2 0 2-AcOEt                                               2-389                                                                             Aze CH═CH                                                                          CH.sub.2 0 2-AcOEt                                               2-390                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-HOEt                                                2-391                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-AcOEt                                               2-392                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-PrnOEt                                              2-393                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-(3-HOOC.PrnO)Et                                     2-394                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-(3-Mec.PrnO)Et                                      2-395                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-BozOEt                                              2-396                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-(cHxCOO)Et                                          2-397                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-HOPr                                                2-398                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-FoOPr                                               2-399                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-AcOPr                                               2-400                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-(3-HOOC.PrnO)Pr                                     2-401                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-(cHxCOO)Pr                                          2-402                                                                             Pip CH═CH                                                                          CH.sub.2 1 3-HOPr                                                2-403                                                                             Pip CH═CH                                                                          CH.sub.2 1 3-AcOPr                                               2-404                                                                             Pip CH═CH                                                                          CH.sub.2 1 3-(3-HOOC.PrnO)Pr                                     2-405                                                                             Pip CH═CH                                                                          CH.sub.2 1 3-BozOPr                                              2-406                                                                             Pip CH═CH                                                                          CH.sub.2 1 3-(cHxCOO)Pr                                          2-407                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-HOBu                                                2-408                                                                             Pip CH═CH                                                                          CH.sub.2 1 2-AcOBu                                               2-409                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-HOEt                                                2-410                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-AcOEt                                               2-411                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-(3-HOOC.PrnO)Et                                     2-412                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-BozOEt                                              2-413                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-(cHxCOO)Et                                          2-414                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 3-HOPr                                                2-415                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 3-AcOPr                                               2-416                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-HOBu                                                2-417                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-AcOBu                                               2-418                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-HOEt                                                2-419                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-AcOEt                                               2-420                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-PrnOE.t                                             2-421                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-(3-HOOC.PrnO)Et                                     2-422                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-BozOEt                                              2-423                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       I 2-(cHxCOO)Et                                          2-424                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-HOPr                                                2-425                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-AcOPr                                               2-426                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-(3-HOOC.PrnO)Pr                                     2-427                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-(cPnCOO)Pr                                          2-428                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-(cHxCOO)Pr                                          2-429                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 3-HOPr                                                2-430                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 3-AcOPr                                               2-431                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-HOBu                                                2-432                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 2-AcOBu                                               2-433                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 2-HOEt                                                2-434                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 2-AcOEt                                               2-435                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 2-(cHxCOO)Et                                          2-436                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 2-HOPr                                                2-437                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 2-AcOPr                                               2-438                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 3-HOPr                                                2-439                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 3-AcOPr                                               2-440                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 2-AcOBu                                               2-441                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 2-HOEt                                                2-442                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 2-AcOEt                                               2-443                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 2-HOPr                                                2-444                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 2-AcOPr                                               2-445                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 3-AcOPr                                               2-446                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 2-AcOBu                                               2-447                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 2-HOEt                                                2-448                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 2-AcOEt                                               2-449                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 2-HOPr                                                2-450                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 2-AcOPr                                               2-451                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 3-HOPr                                                2-452                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 3-AcOPr                                               2-453                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 2-AcOBu                                               2-454                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 2-HOEt                                                2-455                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 2-AcOEt                                               2-456                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 2-HOPr                                                2-457                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 2-AcOPr                                               2-458                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 3-HOPr                                                2-459                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 3-AcOPr                                               2-460                                                                             Pip CH═CH                                                                          CH.sub.2 2 2-HOEt                                                2-461                                                                             Pip CH═CH                                                                          CH.sub.2 2 2-AcOEt                                               2-462                                                                             Pip CH═CH                                                                          CH.sub.2 2 2-PrnOEt                                              2-463                                                                             Pip CH═CH                                                                          CH.sub.2 2 2-(3-HOOC.PrnO)Et                                     2-464                                                                             Pip CH═CH                                                                          CH.sub.2 2 2-BozOEt                                              2-465                                                                             Pip CH═CH                                                                          CH.sub.2 2 2-(cHxCOO)Et                                          2-466                                                                             Pip CH═CH                                                                          CH.sub.2 2 3-HOPr                                                2-467                                                                             Pip CH═CH                                                                          CH.sub.2 2 3-AcOPr                                               2-468                                                                             Pip CH═CH                                                                          CH.sub.2 2 3-(3-HOOC.PrnO)Pr                                     2-469                                                                             Pip CH═CH                                                                          CH.sub.2 2 3-BozOPr                                              2-470                                                                             Pip CH═CH                                                                          CH.sub.2 2 3-(cHxCOO)Pr                                          2-471                                                                             Pip CH═CH                                                                          CH.sub.2 2 2-AcOBu                                               2-472                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 2-HOEt                                                2-473                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 2-AcOEt                                               2-474                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 3-AcOPr                                               2-475                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 3-BozOPr                                              2-476                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 2-AcOBu                                               2-477                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 2-HOEt                                                2-478                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 2-AcOEt                                               2-479                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 3-HOPr                                                2-480                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 3-AcOPr                                               2-481                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 2-AcOBu                                               2-482                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 2-HOEt                                                2-483                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 2-AcOEt                                               2-484                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 3-HOPr                                                2-485                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 3-AcOPr                                               2-486                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 2-AcOBu                                               2-487                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                2 2-HOEt                                                2-488                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                2 2-AcOEt                                               2-489                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                2 2-HOPr                                                2-490                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                2 2-AcOPr                                               2-491                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                2 3-HOPr                                                2-492                                                                             Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                2 3-AcOPr                                               2-493                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 2-HOEt                                                2-494                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 2-AcOEt                                               2-495                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 3-HOPr                                                2-496                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 3-AcOPr                                               2-497                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 2-AcOBu                                               2-498                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 2-HOEt                                                2-499                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 2-AcOEt                                               2-500                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 3-HOPr                                                2-501                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 3-AcOPr                                               2-502                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 2-AcOBu                                               2-503                                                                             Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 2-AcOEt                                               2-504                                                                             Pyr CH═CH                                                                          CH.sub.2 1 2-AcOEt                                               2-505                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 CH.sub.2 OH                                           2-506                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOEt                                                2-507                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-FoOEt                                               2-508                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOEt                                               2-509                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-PrnOEt                                              2-510                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-ByrOEt                                              2-511                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-iByrOEt                                             2-512                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-ValOEt                                              2-513                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-iValOEt                                             2-514                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(PhAcO)Et                                           2-515                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(HOOC.AcO)Et                                        2-516                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-HOOC.PrnO)Et                                     2-517                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-518                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Etc.PrnO)Et                                      2-519                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Prc.PrnO)Et                                      2-520                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Phc.PrnO)Et                                      2-521                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-[3-(4-MePhcO)PrnO]Et                                2-522                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-PhPrnO)Et                                        2-523                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-PhPrnO)Et                                        2-524                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-BozOEt                                              2-525                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(4-MeBozO)Et                                        2-526                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(4-MeOBozO)Et                                       2-527                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(4-FBozO)Et                                         2-528                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(4-ClBozo)Et                                        2-529                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cPrCOO)Et                                          2-530                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cBuCOO)Et                                          2-531                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cPnCOO)Et                                          2-532                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cHxCOO)Et                                          2-533                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOPr                                                2-534                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-FoOPr                                               2-535                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOPr                                               2-536                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-PrnOPr                                              2-537                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-HOOC.PrnO)Pr                                     2-538                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Mec.PrnO)Pr                                      2-539                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Etc.PrnO)Pr                                      2-540                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Phc.PrnO)Et                                      2-541                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-[3-(4-MePhcO)PrnO]Et                                2-542                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(PhAcO)Pr                                           2-543                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-BozOPr                                              2-544                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cPnCOO)Pr                                          2-545                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cHxCOO)Pr                                          2-546                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-HOPr                                                2-547                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-FoOPr                                               2-548                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-AcOPr                                               2-549                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-PrnOPr                                              2-550                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(3-HOOC.PrnO)Pr                                     2-551                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(3-Mec.PrnO)Pr                                      2-552                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(3-Etc.PrnO)Pr                                      2-553                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-BozOPr                                              2-554                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(cPnCOO)Pr                                          2-555                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(cHxCOO)Pr                                          2-556                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOBu                                                2-557                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOBu                                               2-558                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-HOOC.PrnO)Bu                                     2-559                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-BozOBu                                              2-560                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cHxCOO)Bu                                          2-561                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-562                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-FoOEt                                               2-563                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-564                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-PrnOEt                                              2-565                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-ValOEt                                              2-566                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(PhAcO)Et                                           2-567                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Et                                     2-568                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.PrnO)Et                                      2-569                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-Etc.PrnO)Et                                      2-570                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-PhPrnO)Et                                        2-571                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-BozOEt                                              2-572                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(4-MeBozO)Et                                        2-573                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(4-FBozO)Et                                         2-574                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(4-ClBozO)Et                                        2-575                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cPrCOO)Et                                          2-576                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cBuCOO)Et                                          2-577                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Et                                          2-578                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Et                                          2-579                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HOPr                                                2-580                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-FoOPr                                               2-581                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-AcOPr                                               2-582                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-PrnOPr                                              2-583                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Pr                                     2-584                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.PrnO)Pr                                      2-585                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-BozOPr                                              2-586                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Pr                                          2-587                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Pr                                          2-588                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-589                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-590                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-PrnOPr                                              2-591                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-(3-HOOC.PrnO)Pr                                     2-592                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-BozOPr                                              2-593                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-(cPnCOO)Pr                                          2-594                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-(cHxCOO)Pr                                          2-595                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HOBu                                                2-596                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-AcOBu                                               2-597                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Bu                                     2-598                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-BozOBu                                              2-599                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Bu                                          2-600                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-601                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-FoOEt                                               2-602                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-603                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-604                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-ByrOEt                                              2-605                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-iByrOEt                                             2-606                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-ValOEt                                              2-607                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-608                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-Mec.PrnO)Et                                      2-609                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-Etc.PrnO)Et                                      2-610                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(PhAcO)Et                                           2-611                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-612                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(4-MeBozO)Et                                        2-613                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(4-MeOBozO)Et                                       2-614                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(4-FBozO)Et                                         2-615                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(4-ClBozO)Et                                        2-616                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cPrCOO)Et                                          2-617                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cBuCOO)Et                                          2-618                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Et                                          2-619                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-620                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOPr                                                2-621                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOPr                                               2-622                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-PrnOPr                                              2-623                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-624                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-Etc.PrnO)Pr                                      2-625                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-BozOPr                                              2-626                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Pr                                          2-627                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-628                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-629                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-630                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-(3-Mec.PrnO)Pr                                      2-631                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-BozOPr                                              2-632                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-(cHxCOO)Pr                                          2-633                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-634                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-635                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-636                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-BozOBu                                              2-637                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Bu                                          2-638                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-639                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-FoOEt                                               2-640                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-ACOEt                                               2-641                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-PrnOEt                                              2-642                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Et                                     2-643                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(3-Mec.PrnO)Et                                      2-644                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-BozOEt                                              2-645                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Et                                          2-646                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-HOPr                                                2-647                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-AcOPr                                               2-648                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-649                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-BozOPr                                              2-650                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Pr                                          2-651                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-652                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-653                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-654                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-BozOPr                                              2-655                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-(cHxCOO)Pr                                          2-656                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-HOBu                                                2-657                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-658                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-659                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Bu                                          2-660                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-661                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-662                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(3-HOOC.PrnO)Et                                     2-663                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-BozOEt                                              2-664                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Et                                          2-665                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-666                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-667                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-BozOPr                                              2-668                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Pr                                          2-669                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-HOPr                                                2-670                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-671                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-(3-HOOC.PrnO)Pr                                     2-672                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-BozOPr                                              2-673                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-(cHxCOO)Pr                                          2-674                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOBu                                                2-675                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-676                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(3-Etc.PrnO)Bu                                      2-677                                                                             Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Bu                                          2-678                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-679                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-680                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Et                                     2-681                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-BozOEt                                              2-682                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Et                                          2-683                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-HOPr                                                2-684                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-AcOPr                                               2-685                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-686                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-BozOPr                                              2-687                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Pr                                          2-688                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-689                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-690                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-(3-HOOC.PrnO)pr                                     2-691                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-BozOPr                                              2-692                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-(cHxCOO)Pr                                          2-693                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-HOBu                                                2-694                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-AcOBu                                               2-695                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-696                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Bu                                          2-697                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-698                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-699                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Et                                     2-700                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Et                                          2-701                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-HOPr                                                2-702                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-AcOPr                                               2-703                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-704                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Pr                                          2-705                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-706                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-707                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-708                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-(cHxCOO)Pr                                          2-709                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-HOBu                                                2-710                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-AcOBu                                               2-711                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-712                                                                             Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Bu                                          2-713                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOEt                                                2-714                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-FoOEt                                               2-715                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOEt                                               2-716                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-PrnOEt                                              2-717                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-HOOC.PrnO)Et                                     2-718                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-719                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Etc.PrnO)Et                                      2-720                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-BozOEt                                              2-721                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cPnCOO)Et                                          2-722                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cHxCOO)Et                                          2-723                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOPr                                                2-724                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOPr                                               2-725                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-HOOC.PrnO)Pr                                     2-726                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-BozOPr                                              2-727                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cHxCOO)Pr                                          2-728                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-HOPr                                                2-729                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-FoOPr                                               2-730                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-AcOPr                                               2-731                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(3-HOOC.PrnO)Pr                                     2-732                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(3-Mec.PrnO)Pr                                      2-733                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-BozOPr                                              2-734                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-(cHxCOO)Pr                                          2-735                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOBu                                                2-736                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOBu                                               2-737                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-738                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-739                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Et                                     2-740                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.PrnO)Et                                      2-741                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-BozOEt                                              2-742                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Et                                          2-743                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Et                                          2-744                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HOPr                                                2-745                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-AcOPr                                               2-746                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Pr                                     2-747                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Pr                                          2-748                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-749                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-750                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-(cHxCOO)Pr                                          2-751                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HOBu                                                2-752                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-AcOBu                                               2-753                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-754                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-755                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-756                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-757                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-758                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Et                                          2-759                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-760                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOPr                                                2-761                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOPr                                               2-762                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-BozOPr                                              2-763                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-764                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-765                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-766                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-767                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-768                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-769                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-770                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Et                                     2-771                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Et                                          2-772                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-HOPr                                                2-773                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-AcOPr                                               2-774                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-775                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-776                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-HOBu                                                2-777                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-778                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-779                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-780                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-781                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-782                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-HOPr                                                2-783                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-784                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOBu                                                2-785                                                                             Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-786                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-787                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-788                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-HOPr                                                2-789                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-AcOPr                                               2-790                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Pr                                          2-791                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-792                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-793                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-AcOBu                                               2-794                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-795                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-796                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-HOPr                                                2-797                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-AcOPr                                               2-798                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-799                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-800                                                                             Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-AcOBu                                               2-801                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOEt                                                2-802                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOEt                                               2-803                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-PrnOEt                                              2-804                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-HOOC.PrnO)Et                                     2-805                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-806                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-BozOEt                                              2-807                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cHxCOO)Et                                          2-808                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOPr                                                2-809                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-(cHxCOO)Pr                                          2-810                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-HOPr                                                2-811                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-AcOPr                                               2-812                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HOBu                                                2-813                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOBu                                               2-814                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-815                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-816                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-817                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-818                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-819                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-820                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-821                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-822                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-823                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-824                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Pr                                          2-825                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Pr                                          2-826                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-827                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-828                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-829                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-830                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-831                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-832                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-833                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-834                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-835                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-836                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-837                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-838                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-839                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-840                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-841                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-842                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 2-AcOPr                                               2-843                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-844                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-845                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-846                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-847                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-848                                                                             NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-849                                                                             Azi CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOEt                                               2-850                                                                             Aze CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-AcOEt                                               2-851                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 CH.sub.2 OH                                           2-852                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-HOEt                                                2-853                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-FoOEt                                               2-854                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-AcOEt                                               2-855                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-PrnOEt                                              2-856                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-ByrOEt                                              2-857                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-iByrOEt                                             2-858                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-ValOEt                                              2-859                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-iValOEt                                             2-860                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(PhAcO)Et                                           2-861                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(HOOC.AcO)Et                                        2-862                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Hooc.prnO)Et                                     2-863                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-864                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Etc.PrnO)Et                                      2-865                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Prc.PrnO)Et                                      2-866                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Phc.PrnO)Et                                      2-867                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-[3-(4-MePhcO)PrnO]Et                                2-868                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-PhPrnO)Et                                        2-869                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-PhPrnO)Et                                        2-870                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-BozOEt                                              2-871                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(4-MeBozO)Et                                        2-872                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(4-MeOBozo)Et                                       2-873                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(4-FBozO)Et                                         2-874                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(4-ClBozO)Et                                        2-875                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(cPrCOO)Et                                          2-876                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(cBuCOO)Et                                          2-877                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(cPnCOO)Et                                          2-878                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(cHxCoo)Et                                          2-879                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-HOPr                                                2-880                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-FoOPr                                               2-881                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-AcOPr                                               2-882                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-PrnOPr                                              2-883                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-HOOC.PrnO)Pr                                     2-884                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Mec.PrnO)Pr                                      2-885                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Etc.PrnO)Pr                                      2-886                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-Phc.PrnO)Et                                      2-887                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-[3-(4-MePhcO)PrnO]Et                                2-888                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(PhAcO)Pr                                           2-889                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-BozOPr                                              2-890                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(cPnCOO)Pr                                          2-891                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(cHxCOO)Pr                                          2-892                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-HOPr                                                2-893                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-FoOPr                                               2-894                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-AcOPr                                               2-895                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-PrnOPr                                              2-896                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-(3-HOOC.PrnO)Pr                                     2-897                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-(3-Mec.PrnO)Pr                                      2-898                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-(3-Etc.PrnO)Pr                                      2-899                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-BozOPr                                              2-900                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-(cPnCOO)Pr                                          2-901                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 3-(cHxCOO)Pr                                          2-902                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-HOBu                                                2-903                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-AcOBu                                               2-904                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(3-HOOC.PrnO)Bu                                     2-905                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-BozOBu                                              2-906                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 2-(cHxCOO)Bu                                          2-907                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-908                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-FoOEt                                               2-909                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-910                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-PrnOEt                                              2-911                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-ValOEt                                              2-912                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(PhAcO)Et                                           2-913                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Et                                     2-914                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.PrnO)Et                                      2-915                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(3-Etc.PrnO)Et                                      2-916                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(3-PhPrnO)Et                                        2-917                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-BozOEt                                              2-918                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(4-MeBozO)Et                                        2-919                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(4-FBozO)Et                                         2-920                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(4-ClBozO)Et                                        2-921                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(cPrCOO)Et                                          2-922                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(cBuCOO)Et                                          2-923                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Et                                          2-924                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Et                                          2-925                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-HOPr                                                2-926                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-FoOPr                                               2-927                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-AcOPr                                               2-928                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-PrnOPr                                              2-929                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Pr                                     2-930                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.PrnO)Pr                                      2-931                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-BozOPr                                              2-932                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Pr                                          2-933                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Pr                                          2-934                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-935                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-936                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 3-PrnOPr                                              2-937                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 3-(3-HOOC.PrnO)Pr                                     2-938                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 3-BozOPr                                              2-939                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 3-(cPnCOO)Pr                                          2-940                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 3-(cHxCOO)Pr                                          2-941                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-HOBu                                                2-942                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-AcOBu                                               2-943                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Bu                                     2-944                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-BozOBu                                              2-945                                                                             Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Bu                                          2-946                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-947                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-FoOEt                                               2-948                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-949                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-950                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-ByrOEt                                              2-951                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-iByrOEt                                             2-952                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-ValOEt                                              2-953                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-954                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(3-Mec.PrnO)Et                                      2-955                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(3-Etc.PrnO)Et                                      2-956                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(PhAcO)Et                                           2-957                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-958                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(4-MeBozo)Et                                        2-959                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(4-MeOBozO)Et                                       2-960                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(4-FBozO)Et                                         2-961                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(4-ClBozO)Et                                        2-962                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(cPrCOO)Et                                          2-963                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(cBuCOO)Et                                          2-964                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Et                                          2-965                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-966                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-HOPr                                                2-967                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-AcOPr                                               2-968                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-PrnOPr                                              2-969                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-970                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(3-Etc.PrnO)Pr                                      2-971                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-BozOPr                                              2-972                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Pr                                          2-973                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-974                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-975                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-976                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 3-(3-Mec.PrnO)Pr                                      2-977                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 3-BozOPr                                              2-978                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 3-(cHxCOO)Pr                                          2-979                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-980                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-981                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-982                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-BozOBu                                              2-983                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Bu                                          2-984                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-985                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-FoOEt                                               2-986                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-987                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-PrnOEt                                              2-988                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Et                                     2-989                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-(3-Mec.PrnO)Et                                      2-990                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-BozOEt                                              2-991                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Et                                          2-992                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-HOPr                                                2-993                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-AcOPr                                               2-994                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-995                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-BozOPr                                              2-996                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Pr                                          2-997                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-998                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-999                                                                             Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-1000                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 3-BozOPr                                              2-1001                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 3-(cHxCOO)Pr                                          2-1002                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-HOBu                                                2-1003                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-1004                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-1005                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Bu                                          2-1006                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-1007                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-1008                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(3-HOOC.PrnO)Et                                     2-1009                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-BozOEt                                              2-1010                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Et                                          2-1011                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-1012                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-1013                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-BozOPr                                              2-1014                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Pr                                          2-1015                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 3-HOPr                                                2-1016                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-1017                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 3-(3-HOOC.PrnO)Pr                                     2-1018                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 3-BozOPr                                              2-1019                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 3-(cHxCOO)Pr                                          2-1020                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOBu                                                2-1021                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-1022                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(3-Etc.PrnO)Bu                                      2-1023                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH(Me)CH.sub.2                                                                0 2-(cHxCOO)Bu                                          2-1024                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-1025                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-1026                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Et                                     2-1027                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-BozOEt                                              2-1028                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Et                                          2-1029                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-HOPr                                                2-1030                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-AcOPr                                               2-1031                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-1032                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-BozOPr                                              2-1033                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Pr                                          2-1034                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-1035                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-1036                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-1037                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 3-BozOPr                                              2-1038                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 3-(cHxCOO)Pr                                          2-1039                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-HOBu                                                2-1040                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-AcOBu                                               2-1041                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-1042                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Bu                                          2-1043                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-1044                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-1045                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Et                                     2-1046                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Et                                          2-1047                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-HOPr                                                2-1048                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-AcOPr                                               2-1049                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Pr                                     2-1050                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Pr                                          2-1051                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-1052                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-1053                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-1054                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 3-(cHxCOO)Pr                                          2-1055                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-HOBu                                                2-1056                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-AcOBu                                               2-1057                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-(3-HOOC.PrnO)Bu                                     2-1058                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 2-(cHxCOO)Bu                                          2-1059                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-HOEt                                                2-1060                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-FoOEt                                               2-1061                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-AcOEt                                               2-1062                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-PrnOEt                                              2-1063                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(3-HOOC.PrnO)Et                                     2-1064                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(3-Mec.PrnO)Et                                      2-1065                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(3-Etc.PrnO)Et                                      2-1066                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-BozOEt                                              2-1067                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(cPnCOO)Et                                          2-1068                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(cHxCOO)Et                                          2-1069                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-HOPr                                                2-1070                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-AcOPr                                               2-1071                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(3-HOOC.PrnO)Pr                                     2-1072                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-BozOPr                                              2-1073                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(cHxCOO)Pr                                          2-1074                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-HOPr                                                2-1075                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-FoOPr                                               2-1076                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-AcOPr                                               2-1077                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-(3-HOOC.PrnO)Pr                                     2-1078                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-(3-Mec.PrnO)Pr                                      2-1079                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-BozOPr                                              2-1080                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-(cHxCOO)Pr                                          2-1081                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-HOBu                                                2-1082                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-AcOBu                                               2-1083                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-HOEt                                                2-1084                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-AcOEt                                               2-1085                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Et                                     2-1086                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-(3-Mec.Prn.O)Et                                     2-1087                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-BozOEt                                              2-1088                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-(cPnCOO)Et                                          2-1089                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Et                                          2-1090                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-HOPr                                                2-1091                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-AcOPr                                               2-1092                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-(3-HOOC.PrnO)Pr                                     2-1093                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-(cHxCOO)Pr                                          2-1094                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 3-HOPr                                                2-1095                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 3-AcOPr                                               2-1096                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 3-(cHxCOO)Pr                                          2-1097                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-HOBu                                                2-1098                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-AcOBu                                               2-1099                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-HOEt                                                2-1100                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-AcOEt                                               2-1101                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-PrnOEt                                              2-1102                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-(3-HOOC.PrnO)Et                                     2-1103                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-BozOEt                                              2-1104                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-(cPnCOO)Et                                          2-1105                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-(cHxCOO)Et                                          2-1106                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-HOPr                                                2-1107                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-AcOPr                                               2-1108                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-BozOPr                                              2-1109                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 3-HOPr                                                2-1110                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 3-AcOPr                                               2-1111                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 3-(3-HOOC.PrnO)Pr                                     2-1112                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-HOBu                                                2-1113                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 2-AcOBu                                               2-1114                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-HOEt                                                2-1115                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-AcOEt                                               2-1116                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-(3-HOOC.PrnO)Et                                     2-1117                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-(cHxCOO)Et                                          2-1118                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-HOPr                                                2-1119                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-AcOPr                                               2-1120                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 3-HOPr                                                2-1121                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 3-AcOPr                                               2-1122                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-HOBu                                                2-1123                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 2-AcOBu                                               2-1124                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOEt                                                2-1125                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOEt                                               2-1126                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOPr                                                2-1127                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOPr                                               2-1128                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 3-HOPr                                                2-1129                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 3-AcOPr                                               2-1130                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 2-HOBu                                                2-1131                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 2-AcOBu                                               2-1132                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 2-HOEt                                                2-1133                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 2-AcOEt                                               2-1134                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 2-HOPr                                                2-1135                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 2-AcOPr                                               2-1136                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 2-(cHxCOO)Pr                                          2-1137                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 3-HOPr                                                2-1138                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 3-AcOPr                                               2-1139                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 2-AcOBu                                               2-1140                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 2-HOEt                                                2-1141                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 2-AcOEt                                               2-1142                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 2-HOPr                                                2-1143                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 2-AcOPr                                               2-1144                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 3-HOPr                                                2-1145                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 3-AcOPr                                               2-1146                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 2-AcOBu                                               2-1147                                                                            Pip CH═CH                                                                          CH.sub.2 0 2-(nPnCOO)Et                                          2-1148                                                                            Pip CH═CH                                                                          CH.sub.2 0 2-PivOEt                                              2-1149                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-(nPnCOO)Et                                          2-1150                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 2-PivOEt                                              2-1151                                                                            Pyr CH═CH                                                                          CH.sub.2 0 2-(nPnCOO)Et                                          2-1152                                                                            Pyr CH═CH                                                                          CH.sub.2 0 2-PivOEt                                              __________________________________________________________________________

                                      TABLE 3                                     __________________________________________________________________________    Cpd.                                                                          No.                                                                              R.sup.1                                                                           A    B        m R.sup.5                                                __________________________________________________________________________    3-1                                                                              Pip CH═CH                                                                          CH.sub.2 0 Imdazo-2-yl                                            3-2                                                                              Pip CH═CH                                                                          CH.sub.2 0 Imdazo-4-yl                                            3-3                                                                              Pip CH═CH                                                                          CH.sub.2 0 1-Me-Imdazo-2-yl                                       3-4                                                                              Pip CH═CH                                                                          CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-5                                                                              Pip CH═CH                                                                          CH.sub.2 0 5-Me-1,3,4-Oxadiazo-2-yl                               3-6                                                                              Pip CH═CH                                                                          CH.sub.2 0 1,3,4-Thiadiazo-2-yl                                   3-7                                                                              Pip CH═CH                                                                          CH.sub.2 0 5-Me-1,3,4-Thiadiazo-2-yl                              3-8                                                                              Pip CH═CH                                                                          CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-9                                                                              Pip CH═CH                                                                          CH.sub.2 0 1,2,4-Triazo-5-yl                                      3-10                                                                             Pip CH═CH                                                                          CH.sub.2 0 1-Me-1,2,4-Triazo-3-yl                                 3-11                                                                             Pip CH═CH                                                                          CH.sub.2 0 1-Me-1,2,4-Triazo-5-yl                                 3-12                                                                             Pip CH═CH                                                                          CH.sub.2 0 5-Me-1,2,4-Triazo-3-yl                                 3-13                                                                             Pip CH═CH                                                                          CH.sub.2 0 Tetrazo-5-yl                                           3-14                                                                             Pip CH═CH                                                                          CH.sub.2 0 1-Me-Tetrazo-5-yl                                      3-15                                                                             Pip CH═CH                                                                          CH.sub.2 0 Pyz-2-yl                                               3-16                                                                             Pip CH═CH                                                                          CH.sub.2 0 Pyz-3-yl                                               3-17                                                                             Pip CH═CH                                                                          CH.sub.2 0 Pyz-4-yl                                               3-18                                                                             Pip CH═CH                                                                          CH.sub.2 0 3-Me-Pyz-2-yl                                          3-19                                                                             Pip CH═CH                                                                          CH.sub.2 0 2-Me-Pyz-4-yl                                          3-20                                                                             Pip CH═CH                                                                          CH.sub.2 0 3-NHz-Pyz-2-yl                                         3-21                                                                             Pip CH═CH                                                                          CH.sub.2 0 4-NH.sub.2 -Pyz-3-yl                                   3-22                                                                             Pip CH═CH                                                                          CH.sub.2 0 3-NH.sub.2 -Pyz-4-yl                                   3-23                                                                             Pip CH═CH                                                                          CH.sub.2 0 3-HO-Pyz-2-yl                                          3-24                                                                             Pip CH═CH                                                                          CH.sub.2 0 2-HO-Pyz-4-yl                                          3-25                                                                             Pip CH═CH                                                                          CH.sub.2 0 Pymz-2-yl                                              3-26                                                                             Pip CH═CH                                                                          CH.sub.2 0 Pymz-4-yl                                              3-27                                                                             Pip CH═CH                                                                          CH.sub.2 0 4-Me-Pymz-2-yl                                         3-28                                                                             Pip CH═CH                                                                          CH.sub.2 0 5-Me-Pymz-2-yl                                         3-29                                                                             Pip CH═CH                                                                          CH.sub.2 0 2-Me-Pymz-4-yl                                         3-30                                                                             Pip CH═CH                                                                          CH.sub.2 0 5-Me-Pymz-4-yl                                         3-31                                                                             Pip CH═CH                                                                          CH.sub.2 0 6-Me-Pymz-4-yl                                         3-32                                                                             Pip CH═CH                                                                          CH.sub.2 0 2-Me-Pymz-5-yl                                         3-33                                                                             Pip CH═CH                                                                          CH.sub.2 0 4-NH.sub.2 -Pymz-2-yl                                  3-34                                                                             Pip CH═CH                                                                          CH.sub.2 0 5-NH.sub.2 -Pymz-2-yl                                  3-35                                                                             Pip CH═CH                                                                          CH.sub.2 0 2-NH.sub.2 -Pymz-4-yl                                  3-36                                                                             Pip CH═CH                                                                          CH.sub.2 0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-37                                                                             Pip CH═CH                                                                          CH.sub.2 0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-38                                                                             Pip CH═CH                                                                          CH.sub.2 0 5-NH.sub.2 -2-HO-Pymz-4-yl                             3-39                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Imdazo-2-yl                                            3-40                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Imdazo-4-yl                                            3-41                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1-Me-Imdazo-2-yl                                       3-42                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-43                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-Me-1,3,4-Oxadiazo-2-yl                               3-44                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,3,4-Thiadiazo-2-yl                                   3-45                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-Me-1,3,4-Thiadiazo-2-yl                              3-46                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-47                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-5-yl                                      3-48                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1-Me-1,2,4-Triazo-3-yl                                 3-49                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1-Me-1,2,4-Triazo-5-yl                                 3-50                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-Me-1,2,4-Triazo-3-yl                                 3-51                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Tetrazo-5-yl                                           3-52                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1-Me-Tetrazo-5-yl                                      3-53                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pyz-2-yl                                               3-54                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pyz-3-yl                                               3-55                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pyz-4-yl                                               3-56                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-Me-Pyz-2-yl                                          3-57                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-Me-Pyz-4-yl                                          3-58                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-NH.sub.2 -Pyz-2-yl                                   3-59                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-NH.sub.2 -Pyz-4-yl                                   3-60                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-HO-Pyz-2-yl                                          3-61                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HO-Pyz-4-yl                                          3-62                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-63                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-64                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-5-yl                                              3-65                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-Me-Pymz-2-yl                                         3-66                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-2-yl                                         3-67                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-Me-Pymz-4-yl                                         3-68                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-4-yl                                         3-69                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 6-Me-Pymz-4-yl                                         3-70                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-NH.sub.2 -Pymz-2-yl                                  3-71                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-NH.sub.2 -Pymz-2-yl                                  3-72                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-NH.sub.2 -Pymz-4-yl                                  3-73                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-HO-Pymz-5-yl                                         3-74                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-75                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-76                                                                             Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-NH.sub.2 -2-HO-Pymz-4-yl                             3-77                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-78                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-79                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1-Me-Imdazo-2-yl                                       3-80                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-Me-Imdazo-4-yl                                       3-81                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-82                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Me-1,3,4-Oxadiazo-2-yl                               3-83                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Et-1,3,4-Oxadiazo-2-yl                               3-84                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -1,3,4-Oxadiazo-2-yl                        3-85                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-AcNH-1,3,4-Oxadiazo-2-yl                             3-86                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-87                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Me-1,3,4-Thiadiazo-2-yl                              3-88                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -1,3,4-Thiadiazo-2-yl                       3-89                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-90                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-91                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1-Me-1,2,4-Triazo-3-yl                                 3-92                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1-Me-1,2,4-Triazo-5-yl                                 3-93                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Me-1,2,4-Triazo-3-yl                                 3-94                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Cl-1,2,4-Triazo-3-yl                                 3-95                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -1,2,4-Triazo-3-yl                          3-96                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-AcNH-1,2,4-Triazo-3-yl                               3-97                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-98                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1-Me-Tetrazo-5-yl                                      3-99                                                                             Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1-Et-Tetrazo-5-yl                                      3-100                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1-(2-HOEt)-Tetrazo-5-yl                                3-101                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-102                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-3-yl                                               3-103                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-4-yl                                               3-104                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-Me-Pyz-2-yl                                          3-105                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Me-Pyz-2-yl                                          3-106                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-Me-Pyz-4-yl                                          3-107                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-Me-Pyz-4-yl                                          3-108                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-Cl-Pyz-2-yl                                          3-109                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-Cl-Pyz-4-yl                                          3-110                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-2-yl                                   3-111                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pyz-2-yl                                   3-112                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -Pyz-3-yl                                   3-113                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-4-yl                                   3-114                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-HO-Pyz-2-yl                                          3-115                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-HO-Pyz-2-yl                                          3-116                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HO-Pyz-4-yl                                          3-117                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-HO-Pyz-4-yl                                          3-118                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-119                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-120                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-5-yl                                              3-121                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-Me-Pymz-2-yl                                         3-122                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Me-Pymz-2-yl                                         3-123                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-Me-Pymz-4-yl                                         3-124                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Me-Pymz-4-yl                                         3-125                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 6-Me-Pymz-4-yl                                         3-126                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-Cl-Pymz-2-yl                                         3-127                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-Me-Pymz-4-yl                                         3-128                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -Pymz-2-yl                                  3-129                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pymz-2-yl                                  3-130                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -Pymz-4-yl                                  3-131                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pymz-4-yl                                  3-132                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-AcNH-Pymz-2-yl                                       3-133                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-AcNH-Pymz-4-yl                                       3-134                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-135                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-136                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4,6-diNH.sub.2 -Pymz-2-yl                              3-137                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2,5-diNH.sub.2 -Pymz-4-yl                              3-138                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Imdazo-2-yl                                            3-139                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-140                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,3,4-thiadiazo-2-yl                                   3-141                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-142                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-5-yl                                      3-143                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Tetrazo-5-yl                                           3-144                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pyz-2-yl                                               3-145                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pyz-3-yl                                               3-146                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pyz-4-yl                                               3-147                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-148                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-149                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Imdazo-2-yl                                            3-150                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Oxadiazo-2-yl                                    3-151                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Thiadiazo-2-yl                                   3-152                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-3-yl                                      3-153                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-5-yl                                      3-154                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Tetrazo-5-yl                                           3-155                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-2-yl                                               3-156                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-4-yl                                               3-157                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-2-yl                                              3-158                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-4-yl                                              3-159                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Imdazo-2-yl                                            3-160                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-161                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-162                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-163                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-5-yl                                      3-164                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Tetrazo-5-yl                                           3-165                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pyz-2-yl                                               3-166                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pyz-4-yl                                               3-167                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-168                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-169                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Imdazo-2-yl                                            3-170                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo,-2-yl                                   3-171                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-172                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-3-yl                                      3-173                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-174                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Tetrazo-5-yl                                           3-175                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pyz-3-yl                                               3-176                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pyz-4-yl                                               3-177                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-178                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-179                                                                            Pyr CH═CH                                                                          CH.sub.2 0 Imdazo-2-yl                                            3-180                                                                            Pyr CH═CH                                                                          CH.sub.2 0 Imdazo-4-yl                                            3-181                                                                            Pyr CH═CH                                                                          CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-182                                                                            Pyr CH═CH                                                                          CH.sub.2 0 1,3,4-Thiadiazo-2-yl                                   3-183                                                                            Pyr CH═CH                                                                          CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-184                                                                            Pyr CH═CH                                                                          CH.sub.2 0 1,2,4-Triazo-5-yl                                      3-185                                                                            Pyr CH═CH                                                                          CH.sub.2 0 Tetrazo-5-yl                                           3-186                                                                            Pye CH═CH                                                                          CH.sub.2 0 Pyz-2-yl                                               3-187                                                                            Pyr CH═CH                                                                          CH.sub.2 0 Pyz-4-yl                                               3-188                                                                            Pyr CH═CH                                                                          CH.sub.2 0 3-Me-Pyz-2-yl                                          3-189                                                                            Pyr CH═CH                                                                          CH.sub.2 0 2-Me-Pyz-3-yl                                          3-190                                                                            Pyr CH═CH                                                                          CH.sub.2 0 3-NH.sub.2 -Pyz-2-yl                                   3-191                                                                            Pyr CH═CH                                                                          CH.sub.2 0 2-HO-Pyz-3-yl                                          3-192                                                                            Pyr CH═CH                                                                          CH.sub.2 0 Pymz-2-yl                                              3-193                                                                            Pyr CH═CH                                                                          CH.sub.2 0 Pymz-4-yl                                              3-194                                                                            Pyr CH═CH                                                                          CH.sub.2 0 4-Me-Pymz-2-yl                                         3-195                                                                            Pyr CH═CH                                                                          CH.sub.2 0 5-Me-Pymz-2-yl                                         3-196                                                                            Pyr CH═CH                                                                          CH.sub.2 0 2-Me-Pymz-4-yl                                         3-197                                                                            Pyr CH═CH                                                                          CH.sub.2 0 6-Me-Pymz-4-yl                                         3-198                                                                            Pyr CH═CH                                                                          CH.sub.2 0 4-NH.sub.2 -Pymz-2-yl                                  3-199                                                                            Pyr CH═CH                                                                          CH.sub.2 0 4-HO-Pymz-2-yl                                         3-200                                                                            Pyr CH═CH                                                                          CH.sub.2 0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-201                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Imdazo-2-yl                                            3-202                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Imdazo-4-yl                                            3-203                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-204                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,3,4-Thiadiazo-2-yl                                   3-205                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-206                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-5-yl                                      3-207                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Tetrazo-5-yl                                           3-208                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pyz-2-yl                                               3-209                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pyz-4-yl                                               3-210                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-Me-Pyz-2-yl                                          3-211                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-NH.sub.2 -Pyz-2-yl                                   3-212                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-HO-Pyz-2-yl                                          3-213                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-214                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-215                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-5-yl                                              3-216                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-Me-Pymz-2-yl                                         3-217                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-2-yl                                         3-218                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-Me-Pymz-4-yl                                         3-219                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-4-yl                                         3-220                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-NH.sub.2 -Pymz-2-yl                                  3-221                                                                            Pyr CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-HO-Pymz-2-yl                                         3-222                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-223                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-224                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-225                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-226                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-227                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4,-Triazo-5-yl                                     3-228                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-229                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-230                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-3-yl                                               3-231                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-4-yl                                               3-232                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-Me-Pyz-2-yl                                          3-233                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-Me-Pyz-4-yl                                          3-234                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-Cl-Pyz-3-yl                                          3-235                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-2-yl                                   3-236                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-4-yl                                   3-237                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 3-HO-Pyz-2-yl                                          3-238                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-239                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-240                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-Me-Pymz-2-yl                                         3-241                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-Me-Pymz-4-yl                                         3-242                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-Me-Pymz-4-yl                                         3-243                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-Me-Pymz-5-yl                                         3-244                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pymz-2-yl                                  3-245                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -Pymz-4-yl                                  3-246                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-HO-Pymz-4-yl                                         3-247                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-248                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-249                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 4,6-diNH.sub.2 -Pymz-2-yl                              3-250                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Imdazo-2-yl                                            3-251                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-252                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-253                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-254                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-5-yl                                      3-255                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Tetrazo-5-yl                                           3-256                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pyz-2-yl                                               3-257                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pyz-3-yl                                               3-258                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pyz-4-yl                                               3-259                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-260                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-261                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-5-yl                                              3-262                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Imdazo-2-yl                                            3-263                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Oxadiazo-2-yl                                    3-264                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Thiadiazo-2-yl                                   3-265                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-3-yl                                      3-266                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-5-yl                                      3-267                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Tetrazo-5-yl                                           3-268                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-2-yl                                               3-269                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-3-yl                                               3-270                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-2-yl                                              3-271                                                                            Pyr CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-4-yl                                              3-272                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Imdazo-2-yl                                            3-273                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-274                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-275                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-276                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-5-yl                                      3-277                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Tetrazo-5-yl                                           3-278                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pyz-2-yl                                               3-279                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pyz-3-yl                                               3-280                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-281                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-282                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Imdazo-2-yl                                            3-283                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-284                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-285                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-3-yl                                      3-286                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-287                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Tetrazo-5-yl                                           3-288                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pyz-2-yl                                               3-289                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pyz-3-yl                                               3-290                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-291                                                                            Pyr CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-292                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 Imdazo-2-yl                                            3-293                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-294                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 1,3,4-Thiadiazo-2-yl                                   3-295                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-296                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 1,2,4-Triazo-5-yl                                      3-297                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 Tetrazo-5-yl                                           3-298                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 Pyz-2-yl                                               3-299                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 3-Me-Pyz-2-yl                                          3-300                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 Pymz-2-yl                                              3-301                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 4-Me-Pymz-2-yl                                         3-302                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 6-Me-Pymz-4-yl                                         3-303                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-304                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-305                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-5-yl                                      3-306                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pyz-2-yl                                               3-307                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 3-Me-Pyz-2-yl                                          3-308                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-309                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-310                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 4-Me-Pymz-2-yl                                         3-311                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 2-Me-Pymz-4-yl                                         3-312                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-313                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-314                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-315                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-316                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-317                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-318                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-319                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-320                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-321                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-322                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-323                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,2,4-Triazol-3-yl                                     3-324                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-5-yl                                      3-325                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Tetrazo-5-yl                                           3-326                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pyz-2-yl                                               3-327                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-328                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-329                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Oxadiazo-2-yl                                    3-330                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-3-yl                                      3-331                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-5-yl                                      3-332                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-2-yl                                              3-333                                                                            NMe.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-4-yl                                              3-334                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-335                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-336                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-5-yl                                      3-337                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-338                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-339                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-340                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-3-yl                                      3-341                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-342                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-343                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-344                                                                            NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-345                                                                            NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-346                                                                            NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 0 Pymz-2-yl                                              3-347                                                                            NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-348                                                                            NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-349                                                                            NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-350                                                                            NEt.sub.2                                                                         CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-351                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-352                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-353                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-354                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-355                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-356                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-357                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-358                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-359                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-360                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-361                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-362                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-363                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-364                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-365                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-366                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-367                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-368                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-369                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-370                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-371                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-372                                                                            NEt.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-373                                                                            Azi CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-374                                                                            Azi CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-375                                                                            Aze CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-376                                                                            Aze CH═CH                                                                          (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-377                                                                            Pip CH═CH                                                                          CH.sub.2 1 Imdazo-2-yl                                            3-378                                                                            Pip CH═CH                                                                          CH.sub.2 1 1,3,4-Oxadiazo-2-yl                                    3-379                                                                            Pip CH═CH                                                                          CH.sub.2 1 1,3,4-Thiadiazo-2-yl                                   3-380                                                                            Pip CH═CH                                                                          CH.sub.2 1 1,2,4-Triazo-3-yl                                      3-381                                                                            Pip CH═CH                                                                          CH.sub.2 1 1,2,4-Triazo-5-yl                                      3-382                                                                            Pip CH═CH                                                                          CH.sub.2 1 Tetrazo-5-yl                                           3-383                                                                            Pip CH═CH                                                                          CH.sub.2 1 Pyz-2-yl                                               3-384                                                                            Pip CH═CH                                                                          CH.sub.2 1 3-Me-Pyz-2-yl                                          3-385                                                                            Pip CH═CH                                                                          CH.sub.2 1 Pymz-2-yl                                              3-386                                                                            Pip CH═CH                                                                          CH.sub.2 1 4-Me-Pymz-2-yl                                         3-387                                                                            Pip CH═CH                                                                          CH.sub.2 1 6-Me-Pymz-4-yl                                         3-388                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 1,3,4-Oxadiazo-2-yl                                    3-389                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 1,2,4-Triazo-3-yl                                      3-390                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 1,2,4-Triazo-5-yl                                      3-391                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 Pyz-2-yl                                               3-392                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 3-Me-Pyz-2-yl                                          3-393                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 Pymz-2-yl                                              3-394                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 Pymz-4-yl                                              3-395                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 4-Me-Pymz-2-yl                                         3-396                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      1 2-Me-Pymz-4-yl                                         3-397                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Imdazo-2-yl                                            3-398                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Imdazo-4-yl                                            3-399                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 1,3,4-Oxadiazo-2-yl                                    3-400                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 1,3,4-Thiadiazo-2-yl                                   3-401                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 1,2,4-Triazo-3-yl                                      3-402                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 1,2,4-Triazo-5-yl                                      3-403                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Tetrazo-5-yl                                           3-404                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Pyz-2-yl                                               3-405                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Pymz-2-yl                                              3-406                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Pymz-4-yl                                              3-407                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 1,3,4-Oxadiazo-2-yl                                    3-408                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 1,2,4-Triazo-3-yl                                      3-409                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 1,2,4-Triazo-5-yl                                      3-410                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 Tetrazo-5-yl                                           3-411                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 Pyz-2-yl                                               3-412                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 Pymz-2-yl                                              3-413                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       1 Pymz-4-yl                                              3-414                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 1,3,4-Oxadiazo-2-yl                                    3-415                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 1,2,4-Triazo-3-yl                                      3-416                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 1,2,4-Triazo-5-yl                                      3-417                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 Pymz-2-yl                                              3-418                                                                            Pip CH═CH                                                                          CH.sub.2 CH(Me)CH.sub.2                                                                1 Pymz-4-yl                                              3-419                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 1,3,4-Oxadiazo-2-yl                                    3-420                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 1,2,4-Triazo-3-yl                                      3-421                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 1,2,4-Triazo-5-yl                                      3-422                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 Pymz-2-yl                                              3-423                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       1 Pymz-4-yl                                              3-424                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 1,3,4-Oxadiazo-2-yl                                    3-425                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 1,2,4-Triazo-3-yl                                      3-426                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 1,2,4-Triazo-5-yl                                      3-427                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 Pymz-2-yl                                              3-428                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       1 Pymz-4-yl                                              3-429                                                                            Pip CH═CH                                                                          CH.sub.2 2 1,3,4-Oxadiazo-2-yl                                    3-430                                                                            Pip CH═CH                                                                          CH.sub.2 2 1,2,4-Triazo-3-yl                                      3-431                                                                            Pip CH═CH                                                                          CH.sub.2 2 Pymz-2-yl                                              3-432                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 1,3,4-Oxadiazo-2-yl                                    3-433                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 1,2,4-Triazo-3-yl                                      3-434                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 Pymz-2-yl                                              3-435                                                                            Pip CH═CH                                                                          CH.sub.2 CH.sub.2                                                                      2 Pymz-4-yl                                              3-436                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 Imdazo-2-yl                                            3-437                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 Imdazo-4-yl                                            3-438                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 1,3,4-Oxadiazo-2-yl                                    3-439                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 1,3,4-Thiadiazo-2-yl                                   3-440                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 1,2,4-Triazo-3-yl                                      3-441                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 1,2,4-Triazo-5-yl                                      3-442                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 Tetrazo-5-yl                                           3-443                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 Pyz-2-yl                                               3-444                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 Pymz-2-yl                                              3-445                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.3                                                                       2 Pymz-4-yl                                              3-446                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 1,3,4-Oxadiazo-2-yl                                    3-447                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 1,2,4-Triazo-3-yl                                      3-448                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 Pymz-2-yl                                              3-449                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.4                                                                       2 Pymz-4-yl                                              3-450                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 1,3,4-Oxadiazo-2-yl                                    3-451                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 1,2,4-Triazo-3-yl                                      3-452                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 Pymz-2-yl                                              3-453                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.5                                                                       2 Pymz-4-yl                                              3-454                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 1,3,4-Oxadiazo-2-yl                                    3-455                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 1,2,4-Triazo-5-yl                                      3-456                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 Pymz-2-yl                                              3-457                                                                            Pip CH═CH                                                                          (CH.sub.2).sub.6                                                                       2 Pymz-4-yl                                              3-458                                                                            Azi CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 1,2,4-Triazo-3-yl                                      3-459                                                                            Azi CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Pymz-2-yl                                              3-460                                                                            Aze CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 1,2,4-Triazo-3-yl                                      3-461                                                                            Aze CH═CH                                                                          (CH.sub.2).sub.3                                                                       1 Pymz-2-yl                                              3-462                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Imdazo-2-yl                                            3-463                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Imdazo-4-yl                                            3-464                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1-Me-Imdazo-2-yl                                       3-465                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-466                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-Me-1,3,4-Oxadiazo-2-yl                               3-467                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,3,4-Thiadiazo-2-yl                                   3-468                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-Me-1,3,4-Thiadiazo-2-yl                              3-469                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-470                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,2,4-Triazo-5-yl                                      3-471                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1-Me-1,2,4-Triazo-3-yl                                 3-472                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1-Me-1,2,4-Triazo-5-yl                                 3-473                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-Me-1,2,4-Triazo-3-yl                                 3-474                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Tetrazo-5-yl                                           3-475                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1-Me-Tetrazo-5-yl                                      3-476                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pyz-2-yl                                               3-477                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pyz-3-yl                                               3-478                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pyz-4-yl                                               3-479                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-Me-Pyz-2-yl                                          3-480                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-Me-Pyz-4-yl                                          3-481                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-NH.sub.2 -Pyz-2-yl                                   3-482                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-NH.sub.2 -Pyz-3-yl                                   3-483                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-NH.sub.2 -Pyz-4-yl                                   3-484                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-HO-Pyz-2-yl                                          3-485                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HO-Pyz-4-yl                                          3-486                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pymz-2-yl                                              3-487                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pymz-4-yl                                              3-488                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-Me-Pymz-2-yl                                         3-489                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-Me-Pymz-2-yl                                         3-490                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-Me-Pymz-4-yl                                         3-491                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-Me-Pymz-4-yl                                         3-492                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 6-Me-Pymz-4-yl                                         3-493                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-Me-Pymz-5-yl                                         3-494                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-NH.sub.2 -Pymz-2-yl                                  3-495                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-NH.sub.2 -Pymz-2-yl                                  3-496                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-NH.sub.2 -Pymz-4-yl                                  3-497                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-498                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-499                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-NH.sub.2 -2-HO-Pymz-4-yl                             3-500                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Imdazo-2-yl                                            3-501                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Imdazo-4-yl                                            3-502                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1-Me-Imdazo-2-yl                                       3-503                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-504                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-Me-1,3,4-Oxadiazo-2-yl                               3-505                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,3,4-Thiadiazo-2-yl                                   3-506                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-Me-1,3,4-Thiadiazo-2-yl                              3-507                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-508                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-5-yl                                      3-509                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1-Me-1,2,4-Triazo-3-yl                                 3-510                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1-Me-1,2,4-Triazo-5-yl                                 3-511                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-Me-1,2,4-Triazo-3-yl                                 3-512                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Tetrazo-5-yl                                           3-513                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1-Me-Tetrazo-5-yl                                      3-514                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pyz-2-yl                                               3-515                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pyz-3-yl                                               3-516                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pyz-4-yl                                               3-517                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-Me-Pyz-2-yl                                          3-518                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-Me-Pyz-4-yl                                          3-519                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-NH.sub.2 -Pyz-2-yl                                   3-520                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-NH.sub.2 -Pyz-4-yl                                   3-521                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-HO-Pyz-2-yl                                          3-522                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HO-Pyz-4-yl                                          3-523                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-524                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-525                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-5-yl                                              3-526                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-Me-Pymz-2-yl                                         3-527                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-2-yl                                         3-528                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-Me-Pymz-4-yl                                         3-529                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-4-yl                                         3-530                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 6-Me-Pymz-4-yl                                         3-531                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-NH.sub.2 -Pymz-2-yl                                  3-532                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-NH.sub.2 -Pymz-2-yl                                  3-533                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-NH.sub.2 -Pymz-4-yl                                  3-534                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-HO-Pymz-5-yl                                         3-535                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-536                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-537                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-NH.sub.2 -2-HO-Pymz-4-yl                             3-538                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-539                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-540                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1-Me-Imdazo-2-yl                                       3-541                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-Me-Imdazo-4-yl                                       3-542                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-543                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Me-1,3,4-Oxadiazo-2-yl                               3-544                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Et-1,3,4-Oxadiazo-2-yl                               3-545                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -1,3,4-Oxadiazo-2-yl                        3-546                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-AcNH-1,3,4-Oxadiazo-2-yl                             3-547                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-548                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Me-1,3,4-Thiadiazo-2-yl                              3-549                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -1,3,4-Thiadiazo-2-yl                       3-550                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-551                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-552                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1-Me-1,2,4-Triazo-3-yl                                 3-553                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1-Me-1,2,4-Triazo-5-yl                                 3-554                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Me-1,2,4-Triazo-3-yl                                 3-555                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Cl-1,2,4-Triazo-3-yl                                 3-556                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -1,2,4-Triazo-3-yl                          3-557                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-AcNH-1,2,4-Triazo-3-yl                               3-558                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-559                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1-Me-Tetrazo-5-yl                                      3-560                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1-Et-Tetrazo-5-yl                                      3-561                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1-(2-HOEt)-Tetrazo-5-yl                                3-562                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-563                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pyz-3-yl                                               3-564                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pyz-4-yl                                               3-565                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-Me-Pyz-2-yl                                          3-566                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Me-Pyz-2-yl                                          3-567                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-Me-Pyz-4-yl                                          3-568                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-Me-Pyz-4-yl                                          3-569                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-Cl-Pyz-2-yl                                          3-570                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-Cl-Pyz-4-yl                                          3-571                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-2-yl                                   3-572                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pyz-2-yl                                   3-573                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -Pyz-3-yl                                   3-574                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-4-yl                                   3-575                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-HO-Pyz-2-yl                                          3-576                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-HO-Pyz-2-yl                                          3-577                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HO-Pyz-4-yl                                          3-578                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-HO-Pyz-4-yl                                          3-579                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-580                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-581                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-5-yl                                              3-582                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-Me-Pymz-2-yl                                         3-583                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Me-Pymz-2-yl                                         3-584                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-Me-Pymz-4-yl                                         3-585                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Me-Pymz-4-yl                                         3-586                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 6-Me-Pymz-4-yl                                         3-587                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-Cl-Pymz-2-yl                                         3-588                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-Me-Pymz-4-yl                                         3-589                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -Pymz-2-yl                                  3-590                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pymz-2-yl                                  3-591                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -Pymz-4-yl                                  3-592                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pymz-4-yl                                  3-593                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-AcNH-Pymz-2-yl                                       3-594                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-AcNH-Pymz-4-yl                                       3-595                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-596                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-597                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4,6-diNH.sub.2 -Pymz-2-yl                              3-598                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2,5-diNH.sub.2 -Pymz-4-yl                              3-599                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Imdazo-2-yl                                            3-600                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-601                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-602                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-603                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-5-yl                                      3-604                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Tetrazo-5-yl                                           3-605                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pyz-2-yl                                               3-606                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pyz-3-yl                                               3-607                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pyz-4-yl                                               3-608                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-609                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-610                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Imdazo-2-yl                                            3-611                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Oxadiazo-2-yl                                    3-612                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Thiadiazo-2-yl                                   3-613                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-3-yl                                      3-614                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-5-yl                                      3-615                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Tetrazo-5-yl                                           3-616                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-2-yl                                               3-617                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-4-yl                                               3-618                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-2-yl                                              3-619                                                                            Pip CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-4-yl                                              3-620                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Imdazo-2-yl                                            3-621                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-622                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-623                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-624                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-5-yl                                      3-625                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Tetrazo-5-yl                                           3-626                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pyz-2-yl                                               3-627                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pyz-4-yl                                               3-628                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-629                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-630                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Imdazo-2-yl                                            3-631                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-632                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-633                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-3-yl                                      3-634                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-635                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Tetrazo-5-yl                                           3-636                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pyz-3-yl                                               3-637                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pyz-4-yl                                               3-638                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-639                                                                            Pip CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-640                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Imdazo-2-yl                                            3-641                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Imdazo-4-yl                                            3-642                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-643                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,3,4-Thiadiazo-2-yl                                   3-644                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-645                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,2,4-Triazo-5-yl                                      3-646                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Tetrazo-5-yl                                           3-647                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pyz-2-yl                                               3-648                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pyz-4-yl                                               3-649                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-Me-Pyz-2-yl                                          3-650                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-Me-Pyz-3-yl                                          3-651                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-NH.sub.2 -Pyz-2-yl                                   3-652                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-HO-Pyz-3-yl                                          3-653                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pymz-2-yl                                              3-654                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pymz-4-yl                                              3-655                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-Me-Pymz-2-yl                                         3-656                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 5-Me-Pymz-2-yl                                         3-657                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 2-Me-Pymz-4-yl                                         3-658                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 6-Me-Pymz-4-yl                                         3-659                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-NH.sub.2 -Pymz-2-yl                                  3-660                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-HO-Pymz-2-yl                                         3-661                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-662                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Imdazo-2-yl                                            3-663                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Imdazo-4-yl                                            3-664                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-665                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,3,4-Thiadiazo-2-yl                                   3-666                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-667                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-5-yl                                      3-668                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Tetrazo-5-yl                                           3-669                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pyz-2-yl                                               3-670                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pyz-4-yl                                               3-671                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-Me-Pyz-2-yl                                          3-672                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-NH.sub.2 -Pyz-2-yl                                   3-673                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-HO-Pyz-2-yl                                          3-674                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-675                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-676                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-5-yl                                              3-677                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-Me-Pymz-2-yl                                         3-678                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-2-yl                                         3-679                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-Me-Pymz-4-yl                                         3-680                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 5-Me-Pymz-4-yl                                         3-681                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-NH.sub.2 -Pymz-2-yl                                  3-682                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-HO-Pymz-2-yl                                         3-683                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-684                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-685                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-686                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-687                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-688                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-689                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-690                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-691                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pyz-3-yl                                               3-692                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pyz-4-yl                                               3-693                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-Me-Pyz-2-yl                                          3-694                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-Me-Pyz-4-yl                                          3-695                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-Cl-Pyz-3-yl                                          3-696                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-2-yl                                   3-697                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-NH.sub.2 -Pyz-4-yl                                   3-698                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 3-HO-Pyz-2-yl                                          3-699                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-700                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-701                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-Me-Pymz-2-yl                                         3-702                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-Me-Pymz-4-yl                                         3-703                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-Me-Pymz-4-yl                                         3-704                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-Me-Pymz-5-yl                                         3-705                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 5-NH.sub.2 -Pymz-2-yl                                  3-706                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -Pymz-4-yl                                  3-707                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-HO-Pymz-4-yl                                         3-708                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4-NH.sub.2 -5-HO-Pymz-2-yl                             3-709                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 2-NH.sub.2 -5-HO-Pymz-4-yl                             3-710                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 4,6-diNH.sub.2 -Pymz-2-yl                              3-711                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Imdazo-2-yl                                            3-712                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-713                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-714                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-715                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-5-yl                                      3-716                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Tetrazo-5-yl                                           3-717                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pyz-2-yl                                               3-718                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pyz-3-yl                                               3-719                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pyz-4-yl                                               3-720                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-721                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-722                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pymz-5-yl                                              3-723                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Imdazo-2-yl                                            3-724                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Oxadiazo-2-yl                                    3-725                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Thiadiazo-2-yl                                   3-726                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-3-yl                                      3-727                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-5-yl                                      3-728                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Tetrazo-5-yl                                           3-729                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-2-yl                                               3-730                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pyz-3-yl                                               3-731                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-2-yl                                              3-732                                                                            Pyr CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-4-yl                                              3-733                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Imdazo-2-yl                                            3-734                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-735                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-736                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-737                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-5-yl                                      3-738                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Tetrazo-5-yl                                           3-739                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pyz-2-yl                                               3-740                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pyz-3-yl                                               3-741                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-742                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-743                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Imdazo-2-yl                                            3-744                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-745                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-746                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-3-yl                                      3-747                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-748                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Tetrazo-5-yl                                           3-749                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pyz-2-yl                                               3-750                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pyz-3-yl                                               3-751                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-752                                                                            Pyr CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-753                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Imdazo-2-yl                                            3-754                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-755                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,3,4-Thiadiazo-2-yl                                   3-756                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-757                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 1,2,4-Triazo-5-yl                                      3-758                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Tetrazo-5-yl                                           3-759                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pyz-2-yl                                               3-760                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 3-Me-Pyz-2-yl                                          3-761                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 Pymz-2-yl                                              3-762                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 4-Me-Pymz-2-yl                                         3-763                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 0 6-Me-Pymz-4-yl                                         3-764                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-765                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-766                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-5-yl                                      3-767                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pyz-2-yl                                               3-768                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 3-Me-Pyz-2-yl                                          3-769                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-770                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-771                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 4-Me-Pymz-2-yl                                         3-772                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2                                                                      0 2-Me-Pymz-4-yl                                         3-773                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-774                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-775                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-776                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-777                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-778                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-779                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-780                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-781                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-782                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-783                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-784                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-785                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-5-yl                                      3-786                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Tetrazo-5-yl                                           3-787                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pyz-2-yl                                               3-788                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-789                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-790                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Oxadiazo-2-yl                                    3-791                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-3-yl                                      3-792                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-5-yl                                      3-793                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-2-yl                                              3-794                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-4-yl                                              3-795                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-796                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-797                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-5-yl                                      3-798                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-799                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-800                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-801                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-3-yl                                      3-802                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-803                                                                            NMe.sub.2                                                                         CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-804                                                                            NMe.sub.2                                                                         CH═CH                                                                          (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-805                                                                            Azi CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-806                                                                            Azi CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-807                                                                            Aze CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-808                                                                            Aze CH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-809                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 Imdazo-2-yl                                            3-810                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-811                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 1,3,4-Thiadiazo-2-yl                                   3-812                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-813                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 1,2,4-Triazo-5-yl                                      3-814                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 Tetrazo-5-yl                                           3-815                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 Pyz-2-yl                                               3-816                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 3-Me-Pyz-2-yl                                          3-817                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 Pymz-2-yl                                              3-818                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 4-Me-Pymz-2-yl                                         3-819                                                                            Pip CH.sub.2                                                                           CH.sub.2 0 6-Me-Pymz-4-yl                                         3-820                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-821                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-822                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-5-yl                                      3-823                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 Pyz-2-yl                                               3-824                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 3-Me-Pyz-2-yl                                          3-825                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-826                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-827                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 4-Me-Pymz-2-yl                                         3-828                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH.sub.2                                                                      0 2-Me-Pymz-4-yl                                         3-829                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-830                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-831                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-832                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-833                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-834                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-835                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-836                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-837                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-838                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       .0                                                                              Pymz-4-yl                                              3-839                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-840                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-841                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-5-yl                                      3-842                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 Tetrazo-5-yl                                           3-843                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 Pyz-2-yl                                               3-844                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-845                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-846                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 1,3,4-Oxadiazo-2-yl                                    3-847                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-3-yl                                      3-848                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 1,2,4-Triazo-5-yl                                      3-849                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-2-yl                                              3-850                                                                            Pip CH.sub.2                                                                           CH.sub.2 CH(Me)CH.sub.2                                                                0 Pymz-4-yl                                              3-851                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-852                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-853                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-5-yl                                      3-854                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-855                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-856                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-857                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-3-yl                                      3-858                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-859                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-860                                                                            Pip CH.sub.2                                                                           (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-861                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 1,3,4-Oxadiazo-2-yl                                    3-862                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 1,2,4-Triazo-3-yl                                      3-863                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 0 Pymz-2-yl                                              3-864                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 1,3,4-Oxadiazo-2-yl                                    3-865                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 1,2,4-Triazo-3-yl                                      3-866                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 Pymz-2-yl                                              3-867                                                                            Pip (CH.sub.2).sub.3                                                                   CH.sub.2 CH.sub.2                                                                      0 Pymz-4-yl                                              3-868                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 Imdazo-2-yl                                            3-869                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 Imdazo-4-yl                                            3-870                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-871                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 1,3,4-Thiadiazo-2-yl                                   3-872                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-873                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-5-yl                                      3-874                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 Tetrazo-5-yl                                           3-875                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 Pyz-2-yl                                               3-876                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-877                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.3                                                                       0 Pymz-4-yl                                              3-878                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-879                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 1,2,4-Triazo-3-yl                                      3-880                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 Pymz-2-yl                                              3-881                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.4                                                                       0 Pymz-4-yl                                              3-882                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-883                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 1,2,4-Triazo-3-yl                                      3-884                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 Pymz-2-yl                                              3-885                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.5                                                                       0 Pymz-4-yl                                              3-886                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 1,3,4-Oxadiazo-2-yl                                    3-887                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 1,2,4-Triazo-5-yl                                      3-888                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 Pymz-2-yl                                              3-889                                                                            Pip (CH.sub.2).sub.3                                                                   (CH.sub.2).sub.6                                                                       0 Pymz-4-yl                                              3-890                                                                            Pyr CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-891                                                                            Pyr CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              3-892                                                                            Azi CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 1,2,4-Triazo-3-yl                                      3-893                                                                            Aze CH.sub.2                                                                           (CH.sub.2).sub.3                                                                       0 Pymz-2-yl                                              __________________________________________________________________________

Of the compounds listed above, the following are preferred, that is tosay Compounds No. 1-1, 1-5, 1-16, 1-17, 1-19, 1-28, 1-31, 1-45, 1-46,1-47, 1-61, 1-82, 1-87, 1-92, 1-115, 1-116, 1-125, 1-137, 1-166, 1-185,1-216, 1-260, 1-350, 1-462, 1-591, 1-612, 1-951, 1-974, 1-975, 1-976,1-977, 1-981, 1-985, 1-1004, 1-1016, 1-1018, 1-1019, 1-1020, 1-1021,1-1022, 1-1023, 1-1065, 1-1124, 1-1168, 1-1169, 1-1274, 2-2, 2-4, 2-5,2-6, 2-7, 2-8, 2-9, 2-10, 2-12, 2-20, 2-27, 2-28, 2-42, 2-44, 2-57,2-59, 2-96, 2-98, 2-123, 2-209, 2-211, 2-212, 2-216, 2-217, 2-218,2-297, 2-298, 2-390, 2-391, 2-392, 2-461, 2-482, 2-483, 2-493, 2-494,2-506, 2-508, 2-509, 2-852, 2-854, 2-1059, 2-1061, 2-1147, 2-1148, 3-8,3-14, 3-25, 3-79, 3-82, 3-86, 3-87, 3-89, 3-98, 3-100, 3-101, 3-103,3-118, 3-119, 3-121, 3-136, 3-238, 3-405 and 3-579. More preferredcompounds are Compounds No. 1-46, 1-116, 1-137, 1-591, 1-612, 1-974,1-1019, 2-2, 2-4, 2-5, 2-6, 2-7, 2-9, 2-10, 2-12, 2-20, 2-27, 2-28,2-209, 2-211, 2-212, 2-216, 2-217, 2-218, 2-390, 2-392, 2-1147, 2-1148,3-118, 3-238 and 3-579.

The most preferred compounds of the present invention are Compounds No.:

1-116. N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamide;

1-137. 3-amino-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamide;

2-2.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide;

2-4.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide;

2-5.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylthio)acetamide;

2-6.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-butyryloxyethylthio)acetamide;

2-7.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isobutyryloxyethylthio)acetamide;

2-9.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isovaleryloxyethylthio)acetamide;

2-10.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-phenylacetoxyethylthio)acetamide;

2-12.2-{-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]carbamoylmethylthio}ethylhydrogen succinate;

2-20.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-benzoyloxyethylthio)acetamide;

2-27.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclopentylcarbonyloxyethylthio)acetamide;

2-28.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclohexylcarbonyloxyethylthio)acetamide;

2-390.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylsulfinyl)acetamide;

2-392.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylsulfinyl)acetamide;

2-1147.-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(3,3-dimethylbutyryloxy)ethylthio)acetamide;

2-1148.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(2,2-dimethylpropionyloxy)ethylthio)acetamide;

3-118.N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyrimidinylthio)butyramide;

and pharmaceutically acceptable salts thereof.

The compounds of the present invention may be prepared by a variety ofmethods well known in the art for the preparation of compounds of thistype. For example, they may be prepared by the following Reactions A toG: ##STR5##

In the above formulae:

R¹, R², R³, R⁴, R⁵, A, B and m are as defined above;

R^(2a) represents any of the groups defined above for R², except thegroups of formula --NHCHR³ R⁴ (wherein R³ and R⁴ are as defined above)and provided that any hydroxy group in the group represented by R² isprotected;

R^(2b) represents any of the groups defined above for R², except thegroups of formula --NHCHR³ R⁴ (wherein R³ and R⁴ are as defined above);

R^(5a) represents a hydroxyalkyl group having from 2 to 4 carbon atoms(with the proviso that the group must include a moiety having theformula --CH₂ OH);

R⁶ represents an alkyl group having from 1 to 3 carbon atoms andsubstituted with a carboxy or alkoxycarbonyl group having from 1 to 6carbon atoms in the alkoxy moiety;

X represents a halogen atom, preferably a chlorine, bromine or iodineatom;

Y represents a hydrogen atom or an alkali metal atom, such as a lithium,sodium or potassium atom; and

p is an integer from 1 to 3.

Where a hydroxy-protecting group is present, there is no particularlimitation upon the nature of this group, and any such group well knownin the field of organic chemistry may equally be used here. Typicalexamples of such groups include: cyclic ether groups, such as thetetrahydropyranyl, tetrahydrofuranyl and tetrahydrothiopyranyl groups;tri(C₁ -C₄ alkyl)silyl or di(C₁ -C₄ alkyl)arylsilyl groups, such as thetrimethylsilyl, triethylsilyl, t-butyldimethylsilyl andmethyldiphenylsilyl groups; methyl groups substituted with a methoxy,methylthio or trihaloethoxy group, such as the methoxymethyl,methylthiomethyl and 2,2,2-trichloroethoxymethyl groups; and aralkylgroups, such as the benzyl and diphenylmethyl groups. Of these, weparticularly prefer the cyclic ether groups (particularly atetrahydropyranyl group), the substituted silyl groups (particularly atrimethylsilyl or t-butyldimethylsilyl group) and the methoxymethylgroup.

In Reaction A, a compound of formula (Ia), i.e. a compound of formula(I) in which R² represents a group of formula --NHCHR³ R⁴ (wherein R³and R⁴ are as defined above) is prepared by reacting a compound offormula (II) with a compound of formula (III) in the presence ofcarbonyldiimidazole in an inert solvent.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride or chloroform; ethers, such as diethyl ether,tetrahydrofuran or dioxane; amides, such as dimethylformamide,diethylformamide or dimethylacetamide; nitriles, such as acetonitrile;and sulfoxides, such as dimethyl sulfoxide. Of these, we prefer thehalogenated hydrocarbons.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 100° C. (more preferably from 0° C. to50° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 30 minutes to 10 hours (more preferably from 1 to 5hours) will usually suffice.

After completion of the reaction, the desired compound can be recoveredfrom the reaction mixture by conventional means. For example, one suchrecovery method comprises: distilling off the solvent from the reactionmixture or pouring the reaction mixture into water; extracting themixture with a water-immiscible organic solvent; and distilling off theorganic solvent, to leave the desired product as a residue. Ifnecessary, the resulting product can be further purified by conventionalmeans, such as recrystallization, reprecipitation or the variouschromatography techniques, notably column chromatography.

Reaction B comprises another method for preparing a compound of formula(Ia). In this reaction, a compound of formula (Ia) is prepared byreacting a compound of formula (II) with a compound of formula (IV) inan inert solvent.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride or chloroform; ethers, such as diethyl ether,tetrahydrofuran or dioxane; alcohols, such as methanol, ethanol orisopropanol; and nitriles, such as acetonitrile. Of these, we prefer thearomatic hydrocarbons or the halogenated hydrocarbons.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 100° C. (more preferably from 0° C. to50° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 30 minutes to 10 hours (more preferably from 1 to 5hours) will usually suffice.

After completion of the reaction, the desired compound can be recoveredfrom the reaction mixture by conventional means. For example, one suchrecovery method comprises: distilling off the solvent from the reactionmixture or pouring the reaction mixture into water; extracting themixture with a water-immiscible organic solvent; and distilling off theorganic solvent, to leave the desired product as a residue. Ifnecessary, the resulting product can be further purified by conventionalmeans, such as recrystallization, reprecipitation or the variouschromatography techniques, notably column chromatography.

In Reaction C, a compound of formula (Ib), that is a compound of formula(I) wherein R² represents R^(2b) (R^(2b) is as defined above) isprepared by reacting an amine derivative of formula (II) with acarboxylic acid compound of formula (V) or with a reactive derivative ofthe carboxylic acid, and, if desired, removing any hydroxy-protectinggroup.

The reaction of the amine of formula (II) with the carboxylic acid offormula (V) may be carried out in the presence or absence of a base andpreferably in the presence of a condensing agent and of in an inertsolvent.

There is no particular limitation upon the nature of the condensingagent used for the reaction, and any reagent capable of producing anamide bond from a carboxylic acid and an amine may be used. Examples ofthe preferred condensing agents which may be used include:dicyclohexylcarbodiimide (DCC); diethyl cyanophosphonate (DEPC);carbonyldiimidazole; diphenylphosphoryl azide (DPPA);1-hydroxybenzotriazole in admixture with dicyclohexylcarbodiimide; ordiethyl azodicarboxylate in admixture with triphenyl phosphine, Ofthese, we prefer either 1-hydroxybenzotriazole in admixture withdicyclohexylcarbodiimide or diethyl cyanophosphonate.

Examples of preferred bases which may be used include organic amines,such as trimethylamine, triethylamine, pyridine, dimethylaniline,N-methylmorpholine or 4-(N,N-dimethylamino)pyridine. Of these, we prefertriethylamine or N-methylmorpholine.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride, dichloroethane or chloroform; ethers, such asdiethyl ether, tetrahydrofuran or dioxane; esters, such as ethyl acetateor propyl acetate; amides, such as dimethylformamide, dimethylacetamideor hexamethylphosphoric triamide; and nitriles, such as acetonitrile. Ofthese, we prefer the ethers (particularly tetrahydrofuran), halogenatedhydrocarbons (particularly methylene chloride), amides (particularlydimethylformamide) and esters (particularly ethyl acetate).

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -10° C. to 50° C. (more preferably from 0° C. to 30°C.). The time required for the reaction may also vary widely, dependingon many factors, notably the reaction temperature and the nature of thereagents and solvent employed. However, provided that the reaction iseffected under the preferred conditions outlined above, a period of from30 minutes to 24 hours (more preferably from 1 to 15 hours) will usuallysuffice.

Alternatively, the compound of formula (Ib) can be prepared byconverting a carboxylic acid of formula (V) to a reactive derivativethereof, and reacting an amine of formula (II) with the reactivederivative.

Examples of reactive derivatives of the carboxylic acid compoundinclude: acid halides, such as the acid chloride or acid bromide; acidazides; reactive esters, such as esters with N-hydroxybenzotriazole orN-hydroxysuccinimide; acid anhydrides of the carboxylic acid used; andmixed acid anhydrides comprising monoalkyl carbonates in which the alkylgroup has from 1 to 4 carbon atoms (such as monomethyl carbonate,monoethyl carbonate or monoisobutyl carbonate) or monoaryl carbonates(such as monophenyl carbonate or monotolyl carbonate). Of these, weprefer the mixed acid anhydrides with an alkyl carbonate. The reactivederivative of the carboxylic acid, typically an acid halide or an acidanhydride, can be prepared by conventional means. For example, they maybe prepared by reacting a carboxylic acid of formula (V) with anappropriate halide (for example, thionyl chloride, thionyl bromide, acidchloride or acid bromide of the desired carboxylic acid, methylchloroformate, ethyl chloroformate, isobutyl chloroformate, phenylchloroformate or tolyl chloroformate) in an inert solvent (for example,methylene chloride, benzene or tetrahydrofuran) and, if necessary, inthe presence of a base (for example, pyridine, triethylamine ordimethylaniline) in the temperature range from 20° C. to 100° C. for aperiod of from 1 to 20 hours. Other reactive derivatives, such as theacid amide or the reactive ester, can be prepared by reacting thecarboxylic acid of formula (V) with an appropriate compound (forexample, hydrogen azide, N-hydroxybenzotriazole or N-hydroxysuccinimide)in the same manner as described above in Reaction C for producing anamide bond, using a carboxylic acid of formula (V) and an amine offormula (II).

The reaction of the amine of formula (II) and the reactive derivative ofthe carboxylic acid of formula (V) is preferably carried out in thepresence of a solvent. There is no particular restriction on the natureof the solvent to be employed, provided that it has no adverse effect onthe reaction or on the reagents involved and that it can dissolve thereagents, at least to some extent. Examples of suitable solventsinclude: aromatic hydrocarbons, such as benzene, toluene or xylene;halogenated hydrocarbons, especially halogenated aliphatic hydrocarbons,such as methylene chloride, dichloroethane or chloroform; ethers, suchas diethyl ether, tetrahydrofuran or dioxane; and esters, such as ethylacetate. Of these, we prefer the aromatic hydrocarbons or ethers.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -10° C. to 50° C. (more preferably from 0° C. to 25°C.). The time required for the reaction may also vary widely, dependingon many factors, notably the reaction temperature and the nature of thereagents and solvent employed. However, provided that the reaction iseffected under the preferred conditions outlined above, a period of from5 minutes to 20 hours (more preferably from 30 minutes to 10 hours) willusually suffice.

The reaction employed to remove the hydroxy-protecting group will, ofcourse, vary depending upon the nature of the protecting group, but itsremoval may be achieved by conventional means well known in the field oforganic chemistry.

For example, where the protecting group is a silyl group, it can beremoved by reacting the corresponding compound with a base (for example,an alkali metal carbonate, such as sodium carbonate or potassiumcarbonate), an acid (for example, a mineral acid, such as hydrochloricacid or sulfuric acid, or an organic carboxylic acid, such as aceticacid or citric acid) or a fluoride (for example, an ammonium fluoridecompound, such as tributylammonium fluoride) in an inert solvent. Thereaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: ethers,such as diethyl ether, tetrahydrofuran or dioxane; and alcohols, such asmethanol or ethanol. Of these, we prefer the alcohols.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 50° C. (preferably from 0° C. to 30° C.).The time required for the reaction may also vary widely, depending onmany factors, notably the reaction temperature and the nature of thereagents and solvent employed. However, provided that the reaction iseffected under the preferred conditions outlined above, a period of from5 minutes to 2 hours (more preferably from 20 minutes to 1 hour) willusually suffice.

Where the protecting group is a cyclic ether or a substituted methylgroup, it can be removed by reacting the corresponding compound with anacid in an inert solvent. Examples of acids which may be used for thisreaction include: mineral acids, such as hydrochloric acid, hydrobromicacid or sulfuric acid; and organic sulfonic acids, such asmethanesulfonic acid, benzenesulfonic acid or toluenesulfonic acid. Ofthese, we prefer hydrochloric acid or toluenesulfonic acid.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride, dichloroethane or chloroform; ethers, such asdiethyl ether, tetrahydrofuran or dioxane; alcohols, such as methanol orethanol; esters, such as ethyl acetate or propyl acetate; amides, suchas dimethylformamide, dimethylacetamide or hexamethylphosphorictriamide; and nitriles, such as acetonitrile. Of these, we prefer thehalogenated hydrocarbons or esters.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 100° C. (more preferably from 20° C. to70° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 15 minutes to 5 hours (more preferably from 30 minutes to2 hours) will usually suffice.

Where the protecting group is an aralkyl group, it can be removed byreacting the corresponding compound with hydrogen in an inert solvent inthe presence of a catalyst for reduction. Examples of catalysts whichmay be used for reduction include: platinum oxide, platinum black,palladium-on-charcoal, and rhodium-on-charcoal. Of these, we preferpalladium-on-charcoal.

The hydrogen pressure used is normally in the range of from atmosphericpressure to 3 atmospheres pressure.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride, dichloroethane or chloroform; ethers, such asdiethyl ether, tetrahydrofuran or dioxane; alcohols, such as methanol orethanol; esters, such as ethyl acetate or propyl acetate; amides, suchas dimethylformamide, dimethylacetamide or hexamethylphosphorictriamide; and nitriles, such as acetonitrile. Of these, we prefer thealcohols.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 100° C. (more preferably from 10° C. to50° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 15 minutes to 5 hours (more preferably from 30 minutes to2 hours) will usually suffice.

After completion of the reaction, the desired compound from eachreaction can be recovered from the reaction mixture by conventionalmeans. For example, one such method comprises: neutralizing properly thereaction mixture; distilling off the solvent from the reaction mixture;or if necessary, after distilling off the solvent, pouring the reactionmixture into water; extracting the mixture with a water-immiscibleorganic solvent; and distilling off the solvent from the extract, toleave the desired product as a residue. If necessary, the resultingproduct can be further purified by conventional means, such asrecrystallization, reprecipitation or the various chromatographytechniques, notably column chromatography.

In Reaction D, a compound of formula (Ic), that is a compound of formula(I) wherein R² represents a group of formula --B--S(O)_(m) --R⁵ (whereinR⁵, B and m are as defined above), is prepared by reacting a compound offormula (VI) with a compound of formula (VII), normally in an inertsolvent in the presence of a base and then, if desired, oxidizing theresulting thioether compound.

There is no particular restriction on the nature of the base employed inthis reaction, and any base may be used, provided that it has no adverseeffect on any part of the molecule of the reagents. Examples of baseswhich may be used for the reaction include: alkali metal hydroxides,such as sodium hydroxide or potassium hydroxide; alkali metalcarbonates, such as sodium carbonate or potassium carbonate; alkalimetal hydrogencarbonates, such as sodium hydrogencarbonate or potassiumhydrogencarbonate; and organic amines, such as trimethylamine,triethylamine, pyridine, dimethylaniline, N-methylmorpholine or4-(N,N-dimethylamino)pyridine. Of these, we prefer the alkali metalhydroxides.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride or chloroform; ethers, such as diethyl ether,tetrahydrofuran or dioxane; alcohols, such as methanol, ethanol orisopropanol; amides, such as dimethylformamide diethylformamide ordimethylacetamide; nitriles, such as acetonitrile; and sulfoxides, suchas dimethyl sulfoxide. Of these, we prefer the alcohols.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 100° C. (more preferably from 0° C. to50° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 10 minutes to 5 hours (more preferably from 30 minutes to2 hours) will usually suffice.

Oxidation can be conducted by oxidizing the corresponding thioethercompound with an oxidizing reagent in an inert solvent. Examples ofoxidizing reagents which may be used for this reaction include:inorganic peroxides, such as hydrogen peroxide or periodic acid;peroxyaliphatic acids, such as peracetic acid or perpropionic acid;peroxyarylic acids, such as perbenzoic acid or m-chloroperbenzoic acid;and metal salts of peroxyphthalic acids, such as magnesiummonoperoxyphthalate. Of these, we prefer the peroxyarylic acids.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride, dichloroethane or chloroform; and ethers, such asdiethyl ether, tetrahydrofuran or dioxane. Of these, we prefer thehalogenated hydrocarbons.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -30° C. to 50° C. (more preferably from -20° C. toroom temperature). The time required for the reaction may also varywidely, depending on many factors, notably the reaction temperature andthe nature of the reagents and solvent employed. However, provided thatthe reaction is effected under the preferred conditions outlined above,a period of from 10 minutes to 5 hours (more preferably from 30 minutesto 2 hours) will usually suffice.

In this reaction, a sulfinyl compound may be obtained by using about anequimolar of the oxidizing reagent per mole of the thioether compound,and a sulfonyl compound may be obtained by using more than two moles ofthe oxidizing reagent per mole of the thioether compound.

The corresponding thioether compounds of formula (Ib), (Id) or (Ie) canbe subjected to oxidation in a similar manner to that described above toafford the corresponding sulfinyl and sulfonyl compounds.

In the compounds of formula (Ic) where R⁵ represents a hydroxyalkylgroup, if desired, the corresponding acyloxyalkyl compound can beprepared by acylating the hydroxy group.

Specifically, compounds of formula (Ic), wherein R⁵ represents: a C₁ -C₅alkanoyloxy group; a C₂ -C₅ alkanoyloxy group substituted with a C₂ -C₅alkoxycarbonyl, C₇ -C₁₁ aryloxycarbonyl or C₆ -C₁₀ aryl group; a C₇ -C₁₁arylcarbonyloxy group; or an alkyl group substituted with a C₃ -C₆cycloalkylcarbonyloxy group, can be prepared by reacting a hydroxycompound with the corresponding carboxylic acid compound or with areactive derivative thereof.

The reaction conditions used in the reaction of the hydroxy compoundwith the carboxylic acid compound are similar to those used, in thepresence of a condensing agent, in Reaction C, described above.

Reaction of the hydroxy compound with a reactive derivative of thecarboxylic acid compound is preferably conducted in an inert solvent inthe presence or absence of a base.

There is no particular limitation upon the nature of the reactivederivative of the carboxylic acid used, provided that it is a compoundcapable of producing an ester compound by reaction with an alcoholcompound, and it will, of course, depend on the nature of the groupwhich it is desired to introduce. Examples of reactive derivatives whichmay be used for the reaction include: acid halides, such as acetylchloride, propionyl chloride, valeryl chloride, valeryl bromide,isovaleryl chloride, methyl chloroformylacetate, ethyl3-chloroformylpropionate, ethyl 4-chloroformylbutyrate, ethyl5-chloroformylvalerate, phenylacetyl chloride, phenylpropionyl chloride,benzoyl chloride, toluoyl chloride, naphthoyl chloride,cyclopropanecarbonyl chloride, cyclobutanecarbonyl chloride,cyclopentanecarbonyl chloride, and cyclohexanecarbonyl chloride; acidanhydrides, such as acetic formic anhydride, acetic anhydride, propionicanhydride or benzoic anhydride; and mixed acid anhydrides of monoalkylcarbonates (in which the alkyl part has from 1 to 4 carbon atoms), suchas monomethyl carbonate, monoethyl carbonate or monoisobutyl carbonate,or monoaryl carbonates, such as monophenyl carbonate ormono(methylphenyl) carbonate, and of the corresponding acids, such asacetic acid, propionic acid, phenylacetic acid, benzoic acid,cyclopentanecarboxylic acid or cyclohexanecarbonylic acid. Of these, weprefer the acid chlorides, acid anhydrides or mixed acid anhydridescomprising alkyl carbonates. These reactive derivatives of carboxylicacids can be prepared in the same manner as those of carboxylic acidsdescribed in Reaction C, described above.

There is no particular restriction on the nature of the base employed inthis reaction, and any base may be used, provided that it has no adverseeffect on any part of the molecule of the reagents. Examples ofpreferred bases which may be used for this reaction include: organicamines, such as trimethylamine, triethylamine, pyridine,dimethylaniline, N-methylmorpholine or 4-(N,N-dimethylamino)pyridine;and particularly preferably triethylamine or N-methylmorpholine. Anexcess of the organic amine can also serve as a solvent.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride, dichloroethane or chloroform; ethers, such asdiethyl ether, tetrahydrofuran or dioxane; esters, such as ethyl acetateor propyl acetate; amides, such as dimethylformamide, dimethylacetamideor hexamethylphosphoric triamide; and nitriles, such as acetonitrile. Ofthese, we prefer the ethers (particularly tetrahydrofuran) or esters(particularly ethyl acetate).

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -10° C. to 50° C. (more preferably from 0° C. to 30°C.). The time required for the reaction may also vary widely, dependingon many factors, notably the reaction temperature and the nature of thereagents and solvent employed. However, provided that the reaction iseffected under the preferred conditions outlined above, a period of from30 minutes to 24 hours will usually suffice.

Where R⁵ represents an alkyl group substituted with a carboxyl group,the corresponding compounds of formula (Ic) can be prepared by reactinga hydroxy compound with a cyclic carboxylic acid anhydride, such assuccinic anhydride, glutaric anhydride or adipic anhydride (preferablysuccinic anhydride or glutaric anhydride).

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; halogenatedhydrocarbons, especially halogenated aliphatic hydrocarbons, such asmethylene chloride or chloroform; ethers, such as diethyl ether,tetrahydrofuran or dioxane; ketones, such as acetone or methyl ethylketone; amides, such as dimethylformamide, diethylformamide ordimethylacetamide; nitriles, such as acetonitrile; and sulfoxides, suchas dimethyl sulfoxide. Of these, we prefer the ketones.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 100° C. (more preferably from 0° C. to50° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 30 minutes to 8 hours (more preferably from 1 to 5 hours)will usually suffice.

The carboxylic acid compounds obtained above may be converted to thecorresponding ester compounds by conventional esterification procedures,including reacting the carboxylic acid compound with a diazo compound,such as diazomethane, diazoethane, diazopropane, diazobutane ortrimethylsilyldiazomethane in an inert solvent (preferably an ether,such as diethyl ether, tetrahydrofuran or dioxane), at about roomtemperature for a period of from 10 minutes to 2 hours.

After completion of the reaction, the desired compound prepared in thisstep can be recovered from the reaction mixture by conventional means.For example, one such technique comprises: neutralizing properly thereaction mixture; distilling off the solvent from the reaction mixtureor, if necessary, after distilling off the solvent from the reactionmixture, pouring the reaction mixture into water; extracting the mixturewith a water-immiscible organic solvent; and finally distilling off thesolvent from the extract. Further, if necessary, the product can bepurified by conventional means, for example, recrystallization,reprecipitation or the various chromatography techniques, notably columnchromatography.

Reaction E comprises an alternative method for preparing a compound offormula (Ic). In this reaction, a compound of formula (Ic) is preparedby reacting a compound of formula (VIII) with a compound of formula (IX)and, if desired, oxidizing the thioether compound thus obtained. Thisstep is carried out in a similar manner as those described above inReactions C and D.

In Reaction F, a compound of formula (Id), that is, a compound offormula (I) wherein R² represents a group of formula --CH₂ S(O)_(m)(CH₂)_(p+1) OH (wherein m and p are as defined as above), is prepared byreacting a compound of formula (II) with a compound of formula (X),normally in an inert solvent.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene or xylene; ethers, such asdiethyl ether, tetrahydrofuran or dioxane; halogenated hydrocarbons,especially halogenated aliphatic hydrocarbons, such as methylenechloride or chloroform; and alcohols, such as methanol, ethanol orisopropanol. The reaction may also be carried out in the absence of asolvent.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 130° C. (more preferably from 50° C. to100° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 30 minutes to 5 hours (more preferably from 1 to 2 hours)will usually suffice.

After completion of the reaction, the desired compound prepared in thisstep can be recovered from the reaction mixture by conventional means.For example, one such technique comprises: neutralizing properly thereaction mixture; distilling off the solvent from the reaction mixtureor, if necessary, after distilling off the solvent from the reactionmixture, pouring the reaction mixture into water; extracting the mixturewith a water-immiscible organic solvent; and finally distilling off thesolvent from the extract. Further, if necessary, the product can bepurified by conventional means, for example, recrystallization,reprecipitation or the various chromatography techniques, notably columnchromatography.

In Reaction G, a compound of formula (Ie), that is, a compound offormula (I) wherein R² represents a group of formula --B--S(O)_(m)--R^(5a) (wherein R^(5a), B and m are as defined above), can be preparedby reacting a compound of formula (XI) with a reducing reagent in aninert solvent.

Examples of reducing reagents which may be used include: borohydridecompounds, such as lithium borohydride, sodium borohydride, calciumborohydride or sodium cyanoborohydride. Of these, we prefer sodiumborohydride.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: ethers,such as diethyl ether, tetrahydrofuran or dioxane; alcohols, such asmethanol or ethanol; water; or a mixture of any two or more of thesesolvents. Of these, we prefer a mixture of an alcohol and an ether.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Ingeneral, we find it convenient to carry out the reaction at atemperature of from -20° C. to 100° C. (more preferably from 0° C. to30° C.). The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 1 to 24 hours (more preferably from 3 to 10 hours) willusually suffice.

After completion of the reaction, the desired compound prepared in thisstep can be recovered from the reaction mixture by conventional means.For example, one such technique comprises: neutralizing properly thereaction mixture; distilling off the solvent from the reaction mixtureor, if necessary, after distilling off the solvent from the reactionmixture, pouring the reaction mixture into water; extracting the mixturewith a water-immiscible organic solvent; and finally distilling off thesolvent from the extract. Further, if necessary, the product can bepurified by conventional means, for example, recrystallization,reprecipitation or the various chromatography techniques, notably columnchromatography.

The starting materials of formula (II) are known or can be prepared byany of several known methods (for example, as described Japanese PatentKokai Application No. Sho 61-85365 or in an analogous manner).

The starting compounds of formulae (VI), (VIII) and (XI) can be preparedby reacting a compound of formula (II) with a compound of formulaHOCO--B--X, HOCO--B--SY' or HOCO--B--SR⁶, in which: R⁶, B and X are asdefined above; and Y' represents a hydrogen atom, an alkali metal, a C₂-C₅ alkanoyl group (such as an acetyl, propionyl, butyryl or valerylgroup, preferably an acetyl or propionyl group) or an aromatic acylgroup in which the aromatic part has from 6 to 10 ring carbon atoms(such as a benzoyl, toluoyl or naphthoyl group, preferably a benzoylgroup). These reactions may be carried out in a similar manner to thosedescribed in Reaction C described above. Where Y' represents an acylgroup, the compound produced may, if desired, be subjected to hydrolysisusing a base (for example, an alkali metal alkoxide, such as sodiummethoxide or sodium ethoxide, or an alkali metal hydroxide, such assodium hydroxide or potassium hydroxide) at a temperature of from -20°C. to 80° C. (more preferably from 0° C. to 50° C.) in an inert solvent(for example, an alcohol, such as methanol or ethanol) for a suitableperiod, for example from 5 minutes to 10 hours (more preferably from 10minutes to 5 hours) to give a compound in which Y' is a hydrogen atom.

The pyridyloxy derivatives of the present invention have excellenthistamine-H₂ receptor antagonist activity, and are therefore useful forthe prevention and therapy of peptic diseases resulting from undesirablepeptic secretion, such as gastric ulcers, duodenal ulcers, gastritis,esophagistis, gastric dispepsia and Zollinger-Ellison syndrome; they arealso useful for the prophylaxis or treatment of gastric disease beforesurgery.

The compounds of the present invention may be administered in anyconventional form known for use with compounds having this type ofactivity, the precise form depending on the patient and the preferredroute of administration, as is well known in the art. For example, fororal administration they may be formulated as tablets, capsules,granules, powders or syrups; and for parentheral administration they maybe formulated as injections. Depending on the formulation, the compoundsof the present invention may be administered by themselves or inadmixture with conventional additives, such as vehicles (for examplelactose, mannitol, corn starch or crystalline cellulose), binders (forexample cellulose derivatives, gum arabic or gelatin), disintegratingagents (for example calcium carboxymethylcelulose), lubricants (forexample talc or magnesium stearate), stabilizers, corrigents, solventsfor preparing injections (for example water, ethanol or glycerin). Thedosage may vary depending on the age, condition and symptoms of thepatient, as well as the nature and severity of the disorder beingtreated, however, the usual daily dosage for an adult human patientwould be from 1 mg to 1000 mg (preferably from 10 mg to 500 mg), perday, which may be administered as a single dose or divided into severaldoses.

BIOLOGICAL ACTIVITY

The activity of the compounds of the present invention is illustrated bythe following Test Examples. In these, the compounds of the inventionare identified by the number of the subsequent Example in which itspreparation is illustrated. The prior art compounds A, B and C are asidentified in the introductory portion of this specification.

TEST EXAMPLE 1 Atrial Test in Guinea Pigs

The guinea pig right atrium in a spontaneous palpitation was excised,suspended in 40 ml of Krebs-Henselite solution, and a tension of 1 g wasloaded between the atrium preparation and a transducer. The solution wasaerated at a fixed rate at 37° C. 10⁻⁵ M histamine was added, and theheart rate was recorded as control. A test compound was added to aconcentration of 1 μg/ml and then, after 3 minutes, 10⁻⁵ M histamine wasadded, and the heart rate was again recorded. The inhibitory rate (R %)compared to the control group was calculated according to the followingequation:

    R=(1-B/A)×100

where:

A: The heart rate of the control group

B: The heart rate of the group to which the drug was administered

The results are shown in the following Table 4.

                  TABLE 4                                                         ______________________________________                                        Compound of                                                                   Example No.    % Inhibition                                                   ______________________________________                                         1             86                                                              2             90                                                              6             86                                                             13             84                                                             17             83                                                             26             80                                                             34             94                                                             37             99                                                             41             85                                                             48             81                                                             A              68                                                             B              99                                                             C              45                                                             ______________________________________                                    

TEST EXAMPLE 2 Inhibition of Gastric Secretions

This test was carried out according to Shay's method [H. Shay:Gastroenterology 5, 43 (1945)] using male SD rats (5 weeks old). Therats were divided into groups, each group containing 5 rats. The animalswere fasted for 24 hours before the beginning of the experiment. Theywere then anesthetized with ether, the abdominal region was opened, andthe pylorus was ligated. A test compound suspended in a 0.5% w/v aqueouscarboxymethylcellulose (CMC) solution was administered intraduodenally.After 4 hours, the rat was sacrificed by deep anesthesia with ether, andthe stomach was excised. The gastric juice was removed, centrifuged for15 minutes at 2500 rpm, and then 0.1 ml of the supernatant was taken outand titrated until the end point of neutralization with a 0.01N aqueoussolution of sodium hydroxide, to determine the total gastric acidity.The amount of gastric acid secreted per hour (μEq/hr) was calculated,and the inhibition rate (R %) to the control group was calculatedaccording to the following equation.

    R=(1-B/A)×100

where

A: The gastric acid output of the control group (μEq/hr)

B: The amount of gastric acid output of the drug administered group(μEq/hr)

The results are shown in Table 5.

                  TABLE 5                                                         ______________________________________                                        Compound of    Dose                                                           Example No.    (mg/kg)  % Inhibition                                          ______________________________________                                         1             50       63                                                     2             50       52                                                     6             50       73                                                     7             25       63                                                     7             12.5     51                                                    13             50       80                                                    13             25       62                                                    17             50       71                                                    17             25       73                                                    34             25       86                                                    34             12.5     61                                                    37             50       74                                                    41             50       76                                                    41             25       61                                                    48             50       71                                                    58             50       56                                                    A              50       -67                                                   B              50       -40                                                   C              50       56                                                    ______________________________________                                    

TEST EXAMPLE 3 HCl-Ethanol-Induced Ulcer Test in Rats

Male SD rats (6 to 8 weeks old) were fasted for 24 hours before thebeginning of the experiment. Each was then administered orally with 1 mlof a 60% ethanol solution containing 150 mM of hydrogen chloride. After1 hour, the stomach was excised. Into the stomach was injected 10 ml ofa 0.5% formaldehyde solution, and the stomach was fixed for 20 minutes.The injured area (mm²) occuring on the surface of the gastric mucosa wasmeasured, and the total injured area per rat was regarded as the injuryindex.

Test compounds and 0.5% CMC, as the control, were orally administeredeach at a dose of 0.1 ml/100 g, 60 minutes before treatment with theHCl-ethanol solution.

The ulcer formation inhibitory rate (R %) was calculated by thefollowing equation.

    R=(1-B/A)×100

where

A: The injury index of the control group (mm²)

B: The injury index of the drug administered group (mm²)

The results are shown in the following Table 6.

                  TABLE 6                                                         ______________________________________                                        Compound of                                                                   Example No.   % Inhibition*.sup.)                                             ______________________________________                                         2            100                                                              7            61                                                              13            87                                                              34            79                                                              48            78                                                              A             39                                                              B             97                                                              C             56                                                              ______________________________________                                         .sup.*.sup.) Dose: 50 mg/kg.                                             

From these results, it can be seen that the compounds of the presentinvention strongly inhibit ulcer formation in our HCl-ethanol-inducedulcer model, and have a defense factor potentiating activity.

The invention is further illustrated by the following Examples, whichillustrate the preparation of certain of the compounds of the presentinvention, and the subsequent Preparations, which illustrate thepreparation of certain starting materials used in these Examples.

EXAMPLE 1-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide

0.20 ml of 2-mercaptoethanol was added to a solution of 0.24 g of 85%potassium hydroxide (i.e. potassium hydroxide of 85% purity) and 0.94 gof N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-chloroacetamide (prepared as describedin Preparation 1) in 20 ml of methanol, and the resulting mixture wasstirred at room temperature for 1 hour. At the end of this time, thereaction mixture was concentrated by evaporation under reduced pressure.The concentrate was diluted with water, after which it was extractedwith chloroform. The extract was concentrated by evaporation underreduced pressure, and the residue thus obtained was purified by columnchromatography through silica gel, using a 1:9 by volume mixture ofethanol and chloroform as the eluent, to give 0.95 g (yield 90%) of thetitle compound as an oil.

Nuclear Magnetic Resonance. Spectrum (CDCl₃), δ ppm: 1.32-1.52 (2H,multiplet); 1.52-1.70 (4H, multiplet); 2.25-2.55 (4H, multiplet); 2.77(2H, triplet, J=6.3 Hz); 3.25-3.50 (1H, broad); 3.27 (2H, singlet); 3.44(2H, singlet); 3.80 (2H, triplet, J=6.3 Hz); 4.05 (2H, triplet, J=6.1Hz); 4.93 (2H, doublet, J=6.8 Hz); 5.68-5.80 (1H, multiplet); 5.80-5.95(1H, multiplet); 6.79 (1H, singlet); 6.90 (1H, doublet, J=5.4 Hz);7.08-7.28 (1H, broad); 8.06 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3360, 2920, 1650,1610, 1415, 1400, 1295, 1285, 1030.

EXAMPLE 2N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide

0.50 g of N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide (prepared as describedin Example 1) was added to a mixture of 0.47 ml of acetic anhydride and0.39 g of pyridine, and the resulting mixture was heated at 60° C. for 2hours. At the end of this time, the reaction mixture was poured intoice-water, after which a saturated aqueous solution of sodiumhydrogencarbonate was added. The aqueous mixture was then extracted withchloroform. The extract was concentrated by evaporation under reducedpressure, and the residue was purified by column chromatography throughsilica gel, using a 1:19 by volume mixture of methanol and methylenechloride as the eluent, to give 0.51 g (yield 91%) of the title compoundas an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.50 (2H,multiplet); 1.50-1.70 (4H, multiplet); 2.06 (3H, singlet); 2.30-2.45(4H, multiplet); 2.79 (2H, triplet, J=6.3 Hz); 3.28 (2H, singlet); 3.41(2H, singlet); 4.08 (2H, triplet, J=6.3 Hz); 4.23 (2H, triplet, J=6.3Hz); 4.94 (2H, doublet, J=6.8 Hz); 5.62-5.74 (1H, multiplet); 5.82-5.95(1H, multiplet); 6.74 (1H, singlet); 6.88 (1H, doublet, J=5.4 Hz);6.90-7.05 (1H, broad); 8.06 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3370, 2920, 1735,1660, 1610, 1515, 1415, 1400, 1295, 1285, 1025.

The hydrochloride of the title compound, melting at 198°-208° C., wasprepared by dissolving the compound obtained above in ethyl acetate,after which it was treated with an excess of a 4N ethyl acetate solutionof hydrogen chloride.

The oxalate of the title compound, melting at 127°-133° C., was preparedby dissolving the title compound, obtained as described above, inacetone, after which an equimolar amount of oxalic acid was added, andcrystals of the oxalate, which precipitated, were collected byfiltration.

EXAMPLE 3N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-hydroxyethylthio)butyramide

Following a procedure similar to that described in Example 1, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 2-mercaptoethanol as starting materials, in relative proportionssimilar to those used in that Example, and carrying out the reaction at80° C. for 5 hours, the title compound was obtained in a 66% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃) δ ppm: 1.35-1.50 (2H,multiplet); 1.50-1.75 (4H, multiplet); 1.80-2.02 (2H, multiplet);2.30-2.50 (4H, multiplet); 2.32 (2H, triplet, J=7.0 Hz); 2.50-2.65 (1H,singlet); 2.59 (2H, triplet, J=7.0 Hz); 2.72 (2H, triplet, J=6.7 Hz);3.44 (2H, singlet); 3.68-3.80 (2H, multiplet); 4.03 (2H, triplet, J=6.8Hz); 4.93 (2H, doublet, J=6.8 Hz); 5.60-5.75 (1H, multiplet); 5.75-5.90(1H, multiplet); 6.10-6.30 (1H, broad); 6.76 (1H, singlet); 6.90 (1H,doublet, J=5.4 Hz); 8.05 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3440, 2930, 1660,1610, 1415, 1400, 1295, 1285, 1030.

EXAMPLE 4N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxypropylthio)acetamide

Following a procedure similar to that described in Example 1, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenyl]-2-chloroacetamide(prepared as described in Preparation 1) and 1-mercapto-2-propanol asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in an 89% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.25 (3H, doublet,J=6.4 Hz); 1.30-1.86 (1H, broad); 1.38-1.49 (2H, multiplet); 1.53-1.65(4H, multiplet); 2.31-2.43 (4H, multiplet); 2.54 (1H, doublet ofdoublets, J=8.3 & 13.9 Hz); 2.74 (1H, doublet of doublets, J=3.4 & 13.9Hz); 3.25 (1H, doublet, J=16.1 Hz); 3.29 (1H, doublet, J=16.1 Hz); 3.41(2H, singlet); 3.87-4.01 (1H, multiplet); 4.06 (2H, doublet, J=6.1 Hz);4.93 (2H, doublet, J=6.8 Hz); 5.65-5.77 (1H, multiplet); 5.83-5.93 (1H,multiplet); 6.75 (1H, singlet); 6.89 (1H, doublet, J=5.4 Hz); 7.03-7.21(1H, broad); 8.05 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (liquid film), ν_(max) cm⁻¹ : 3293, 2935,1648, 1613, 1560, 1421, 1403, 1301, 1290, 1039.

EXAMPLE 5 N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-hydroxypropylthio)butyramide

Following a procedure similar to that described in Example 1, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 1-mercapto-2-propanol as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained in a 58% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.24 (3H, doublet,J=6.6 Hz); 1.38-1.50 (2H, multiplet); 1.52-1.64 (4H, multiplet);1.84-2.04 (2H, multiplet); 2.27-2.46 (6H, multiplet); 2.46 (1H, doubletof doublets, J=5.3 & 13.9 Hz); 2.59 (2H, triplet, J=6.9 Hz); 2.71 (1H,doublet of doublets, J=3.3 & 13.9 Hz); 3.41 (2H, singlet); 3.81-3.92(1H, multiplet); 4.03 (2H, triplet, J=5.9 Hz); 4.93 (2H, doublet, J=6.6Hz); 5.78-5.91 (1H, multiplet); 5.63-5.76 (1H, multiplet); 6.06-6.22(1H, broad); 6.74 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.04 (1H,doublet, J=5.3 Hz).

Infrared Absorption Spectrum (liquid film), ν_(max) cm⁻¹ : 3298, 2935,1647, 1613, 1560, 1421, 1403, 1311, 1301, 1289, 1070.

EXAMPLE 6N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-acetoxyethylthio)butyramide

Following a procedure similar to that described in Example 2, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-hydroxyethylthio)butyramide (prepared as describedin Example 3) and acetic anhydride as starting materials, in relativeproportions similar to those used in that Example, the title compound,melting at 36°-40° C., was obtained in an 80% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.30-1.60 (2H,multiplet); 1.60-1.80 (4H, multiplet); 1.80-2.02 (2H, multiplet); 2.06(3H, singlet); 2.32 (2H, triplet, J=7.0 Hz); 2.30-2.55 (4H, multiplet);2.62 (2H, triplet, J=7.0 Hz); 2.73 (2H, triplet, J=6.8 Hz); 3.46 (2H,singlet); 4.04 (2H, triplet, J=6.1 Hz); 4.20 (2H, triplet, J=6.8 Hz);4.93 (2H, doublet, J=6.8 Hz); 5.60-5.75 (1H, multiplet); 5.77-5.90 (1H,multiplet); 6.00-6.20 (1H, broad); 6.75 (1H, singlet); 6.92 (1H,doublet, J=5.4 Hz); 8.06 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3450, 2930, 1735,1665, 1610, 1415, 1400, 1295, 1285, 1030.

EXAMPLE 7N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylthio)acetamide

0.09 ml of propionyl chloride was added to a mixture of 0.40 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide (prepared as describedin Example 1) and 1.02 ml of pyridine, and the resulting mixture wasallowed to stand at room temperature for 2 hours. At the end of thistime, the reaction mixture was poured into ice-water, and a saturatedaqueous solution of sodium hydrogencarbonate was added to the resultingmixture, after which it was extracted with chloroform. The extract wasconcentrated by evaporation under reduced pressure and the residue waspurified by column chromatography through silica gel, using a 1:19 byvolume mixture of methanol and ethyl acetate as the eluent, to give 0.39g (yield 85%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.14 (3H, triplet,J=7.5 Hz); 1.35-1.75 (6H, multiplet); 2.30-2.60 (4H, multiplet); 2.34(2H, quartet, J=7.5 Hz); 2.79 (2H, triplet, J=6.6 Hz); 3.28 (2H,singlet); 3.41 (2H, singlet); 4.08 (2H, triplet, J=6.6 Hz); 4.25 (2H,triplet, J=6.3 Hz); 4.93 (2H, doublet, J=6.6 Hz); 5.63-5.69 (1H,multiplet); 5.72-5.93 (1H, multiplet); 6.73 (1H, singlet); 6.88 (1H,doublet, J=5.3 Hz); 6.95-7.10 (1H, broad); 8.06 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3380, 2940, 1735,1665, 1615, 1420, 1405, 1300, 1290, 1180.

The hydrochloride of the title compound, melting at 99°-106° C., wasprepared by dissolving the title compound, prepared as described above,in diethyl ether, after which the resulting solution was treated with anequimolar amount of a 4N ethyl acetate solution of hydrogen chloride.

Nuclear Magnetic Resonance Spectrum (CDCl₃ +CD₃ OD), δ ppm: 1.10 (3H,triplet, J=7.6 Hz); 1.58-1.76 (2H, multiplet); 1.76-1.94 (4H,multiplet); 2.35 (2H, quartet, J=7.6 Hz); 2.84 (2H, triplet, J=6.6 Hz);3.03-3.38 (4H, multiplet); 3.24 (2H, singlet); 3.99 (2H, triplet, J=6.6Hz); 4.24 (2H, triplet, J=6.6 Hz); 4.26 (2H, singlet); 4.99 (2H,doublet, J=6.6 Hz); 5.59-5.70 (1H, multiplet); 5.76-5.86 (1H,multiplet); 7.00 (1H, singlet); 7.10 (1H, doublet, J=5.0 Hz); 8.25 (1H,doublet, J=5.0 Hz).

The dihydrochloride of the title compound, melting at 235°-255° C., wasprepared by dissolving the title compound, prepared as described above,in ethyl acetate, after which the resulting solution was treated with amolar excess of a 4N ethyl acetate solution of hydrogen chloride.

Nuclear Magnetic Resonance Spectrum (CDCl₃ +CD₃ OD), δ ppm: 1.10 (3H,triplet, J=7.6 Hz); 1.44-1.69 (2H, multiplet); 1.75-2.05 (4H,multiplet); 2.35 (2H, quartet, J=7.6 Hz); 2.84 (2H, triplet, J=6.6 Hz);2.98-3.19 (2H, multiplet); 4.00 (2H, triplet, J=5.9 Hz); 4.24 (2H,triplet, J=6.6 Hz); 4.49 (2H, singlet); 5.18 (2H, doublet, J=5.9 Hz);5.66-5.88 (2H, multiplet); 7.48 (1H, doublet, J=5.3 Hz); 7.66 (1H,singlet); 8.39 (1H, doublet, J=5.3 Hz).

EXAMPLE 82-{N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]carbamoylmethylthio}ethylhydrogen succinate

0.11 g of succinic anhydride was added to a solution of 0.4 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide (prepared as describedin Example 1) in 10 ml of acetone, and the resulting mixture was stirredat room temperature for 3 hours. At the end of this time, the reactionmixture was concentrated by evaporation under reduced pressure, and theconcentrate was purified by column chromatography through silica gel,using a 100:5:2 by volume mixture of methylene chloride, triethylamineand methanol as the eluent, to give 0.49 g of the triethylamine salt ofthe title compound in an 80% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.18 (9H, triplet,J=7.3 Hz); 1.40-1.55 (2H, multiplet); 1.55-1.80 (4H, multiplet);2.40-2.60 (2H, multiplet); 2.50-2.68 (4H, multiplet); 2.78 (2H, triplet,J=6.3 Hz); 2.82 (6H, quartet, J=7.3 Hz); 3.50 (2H, singlet); 4.08 (2H,triplet, J=6.3 Hz); 4.26 (2H, triplet, J=6.3 Hz); 4.40-5.10 (1H, broad);4.93 (2H, doublet, J=7.2 Hz); 5.66-5.75 (1H, multiplet); 5.82-5.95 (1H,multiplet); 6.79 (1H, singlet); 6.87 (1H, doublet, J=5.2 Hz); 8.08 (1H,doublet, J=5.2 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3380, 1735, 1660,1610, 1415, 1400, 1295, 1285, 1160, 1030.

EXAMPLE 9N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-benzoyloxyethylthio)acetamide

0.24 ml of benzoyl chloride was added, whilst ice-cooling, to a mixtureof 0.40 g of N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide (preparedas described in Example 1) and 1.02 ml of pyridine, and the resultingmixture was stirred at room temperature for 2 hours. At the end of thistime, the mixture was concentrated by evaporation under reducedpressure. The concentrate was diluted with water and made alkaline bythe addition of an aqueous ammonia solution, after which it wasextracted with ethyl acetate. The extract was concentrated byevaporation under reduced pressure, and the concentrate was purified bycolumn chromatography through silica gel, using a 1:40 by volume mixtureof methanol and ethyl acetate as the eluent, to give 0.31 g of the titlecompound in a 61% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.35-1.50 (2H,multiplet); 1.50-1.75 (4H, multiplet); 2.25-2.45 (4H, multiplet); 2.94(2H, triplet, J=6.3 Hz); 3.40 (2H, singlet); 3.32 (2H, singlet); 4.07(2H, triplet, J=6.3 Hz); 4.49 (2H, triplet, J=6.6 Hz); 4.92 (2H,doublet, J=6.6 Hz); 5.62-5.71 (1H, multiplet); 5.81-5.88 (1H,multiplet); 6.73 (1H, singlet); 6.87 (1H, doublet, J=5.3 Hz); 7.40-7.62(4H, multiplet); 8.02-8.07 (3H, multiplet).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3390, 2940, 1720,1665, 1615, 1275, 1170.

The dihydrochloride of the title compound, melting at 185°-195° C., wasprepared by dissolving the compound obtained above in ethyl acetate,after which the resulting solution was treated with a molar excess of a4N ethyl acetate solution of hydrogen chloride.

EXAMPLE 10N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclohexylcarbonyloxyethylthio)acetamide

0.10 ml of ethyl chloroformate was added, whilst ice-cooling, to asolution of 0.13 ml of cyclohexanecarboxylic acid in 18 ml of ethylacetate, and the resulting mixture was stirred at room temperature for 1hour. At the end of this time, a solution of 0.40 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide(prepared as described in Example 1) in 4 ml of ethyl acetate was addedto the reaction mixture, whilst ice-cooling. The reaction mixture wasthen stirred at room temperature for 1 hour, after which it was heatedunder reflux for 16 hours. At the end of this time, it was concentratedby evaporation under reduced pressure. The concentrate was purified bycolumn chromatography through silica gel, using a 1:9 by volume mixtureof methanol and ethyl acetate as the eluent, to give 0.18 g of the titlecompound in a 35% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.17-2.09 (16H,multiplet); 2.23-2.47 (5H, multiplet); 2.79 (2H, triplet, J=6.3 Hz);3.28 (2H, singlet); 3.42 (2H, singlet); 4.08 (2H, triplet, J=6.3 Hz);4.23 (2H, triplet, J=6.3 Hz); 4.94 (2H, doublet, J=6.6 Hz); 5.81-5.94(1H, multiplet); 5.62-5.74 (1H, multiplet); 6.74 (1H, singlet);6.85-7.05 (1H, broad); 6.89 (1H, doublet, J=5.3 Hz); 8.06 (1H, doublet,J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3380, 2940, 1730,1665, 1610, 1310, 1165.

EXAMPLE 11 N-[4-(4-Piperidinomethyl-2 -pyridyloxy)-cis-2-butenyl]-3-(2-hydroxyethylthio)propionamide

105 mg of sodium hydride (as a 55% w/w dispersion in mineral oil) wereadded, whilst ice-cooling and in an atmosphere of nitrogen, to asolution of 0.76 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-3-mercaptopropionamide(prepared as described in Preparation 3) in 24 ml of dimethylformamide,and the resulting mixture was stirred at room temperature for 30minutes. At the end of this time, 0.16 ml of ethylene chlorohydrin wereadded to the reaction mixture, whilst ice-cooling. The reaction mixturewas stirred at room temperature for 15 minutes, after which it waspoured into ice-water and extracted with ethyl acetate. The extract wasconcentrated by evaporation under reduced pressure, and the residue thusobtained was purified by column chromatography through silica gel, usinga 1:9 by volume mixture of methanol and methylene chloride as theeluent, to give 0.56 g of the title compound as an oil in a 65% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.50 (2H,multiplet); 1.50-1.64 (4H, multiplet); 1.55-2.10 (1H, broad); 2.30-2.43(4H, multiplet); 2.49 (2H, triplet, J=6.9 Hz); 2.74 (2H, triplet, J=5.9Hz); 2.88 (2H, triplet, J=6.9 Hz); 3.41 (2H, singlet); 3.76 (2H, doubletof triplets, J=5.3 & 5.9 Hz); 4.05 (2H, triplet, J=6.3 Hz); 4.93 (2H,doublet, J=6.6 Hz); 5.63-5.78 (1H, multiplet); 5.78-5.90 (1H,multiplet); 6.75 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.04 (1H,doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 2930, 1665,1612, 1418, 1400, 1300, 1290, 1035.

EXAMPLE 12N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-3-(2-acetoxyethylthio)propionamide

Following a procedure similar to that described in Example 2, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-3-(2-hydroxyethylthio)propionamide(prepared as described in Example 11) and acetic anhydride as startingmaterials, in relative proportions similar to those used in thatExample, the title compound was obtained in an 87% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.50 (2H,multiplet); 1.50-1.63 (4H, multiplet); 2.07 (3H, singlet); 2.28-2.43(4H, multiplet); 2.48 (3H, triplet, J=7.3 Hz); 2.77 (2H, triplet, J=6.9Hz); 3.41 (2H, singlet); 4.05 (2H, triplet, J=6.3 Hz); 4.22 (2H,triplet, J=6.9 Hz); 4.93 (2H, doublet, J=6.6 Hz); 5.62-5.76 (1H,multiplet); 5.79-5.90 (1H, multiplet); 6.17-6.40 (1H, broad); 6.74 (1H,singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.04 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3450, 2930, 1735,1665, 1610, 1415, 1400, 1298, 1288, 1028.

EXAMPLE 13N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamide

A solution of 2.39 g of 4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine and 1.08 g of 4-pyrazolecarboxylic acid in 40 ml ofdry dimethylformamide was stirred for 5 minutes, whilst ice-cooling.1.89 g of diethyl cyanophosphonate and 1.65 ml of triethylamine wereadded to the mixture, and the resulting mixture was stirred at roomtemperature for 3 hours. At the end of this time, the reaction mixturewas diluted with water and extracted with ethyl acetate. The extract waswashed with a saturated aqueous solution of sodium hydrogencarbonate andthen with a saturated aqueous solution of sodium chloride, after whichit was dried over anhydrous magnesium sulfate. The solvent was thenremoved by distillation under reduced pressure, and the residue waspurified by column chromatography through silica gel, using a 1:9 byvolume mixture of methanol and chloroform as the eluent, to give 1.65 g(yield 51%) of the title compound as a white powder, melting at121°-123° C.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.52 (2H,multiplet); 1.52-1.66 (4H, multiplet); 2.32-2.48 (4H, multiplet); 3.42(2H, singlet); 4.16 (2H, triplet, J=5.6 Hz); 4.95 (2H, doublet, J=5.9Hz); 5.72-5.96 (2H, multiplet); 6.74 (1H, singlet); 6.81 (1H, broadtriplet, J=5.6 Hz); 6.87 (1H, doublet, J=5.3 Hz); 7.99 (2H, singlet);8.03 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 2933, 1629, 1611,1566, 1530, 1408, 1342, 1299.

EXAMPLE 14

N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]thiophene-2-carboxamide

240 mg of 2-thiophenecarboxylic acid, 390 mg ofN,N'-dicyclohexylcarbodiimide and 275 mg of 1-hydroxybenzotriazole wereadded to a solution of 485 mg of4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine in 10 ml of drydimethylformamide, and the resulting mixture was stirred at roomtemperature for 17 hours. At the end of this time, the reaction mixturewas mixed with ethyl acetate, and the urea which precipitated wasremoved by filtration. The filtrate was diluted with water and extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium hydrogencarbonate and then with a saturated aqueoussolution of sodium chloride, after which it was dried over anhydrousmagnesium sulfate. The solvent was then removed by distillation underreduced pressure, and the residue was purified by column chromatographythrough silica gel, using a 1:19 by volume mixture of methanol andmethylene chloride as the eluent, to give 499 mg (yield 73%) of thetitle compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.52 (2H,multiplet); 1.52-1.65 (4H, multiplet); 2.28-2.46 (4H, multiplet); 3.41(2H, singlet); 4.22 (2H, triplet, J=6.3 Hz); 4.98 (2H, doublet, J=6.6Hz); 5.73-5.85 (1H, multiplet); 5.85-5.97 (1H, multiplet); 6.56 (1H,broad singlet); 6.74 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz);7.02-7.09 (1H, multiplet); 7.46 (1H, doublet, J=5.3 Hz); 7.51 (1H,doublet, J=4.0 Hz); 8.03 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2920, 1665, 1640,1610, 1565, 1530, 1500, 1415, 1400, 1295, 1285.

The hydrochloride of the title compound, melting at 180°-183° C., wasprepared by dissolving the title compound obtained above in ethylacetate, after which it was treated with an equimolar amount of an ethylacetate solution of hydrogen chloride.

EXAMPLE 15N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrrole-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine and2-pyrrolecarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas colorless prisms, melting at 136°-137° C., in an 80% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.51 (2H,multiplet); 1.51-1.65 (4H, multiplet); 2.33-2.48 (4H, multiplet); 3.42(2H, singlet); 4.21 (2H, triplet, J=6.4 Hz); 4.98 (2H, doublet, J=6.3Hz); 5.70-5.79 (1H, multiplet); 5.83-5.92 (1H, multiplet); 6.20-6.23(1H, multiplet); 6.25-6.36 (1H, broad); 6.52-6.55 (1H, multiplet); 6.75(1H, singlet); 6.88-6.93 (2H, multiplet); 8.06 (1H, doublet, J=4.9 Hz);9.51-9.75 (1H, broad).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3242, 1641, 1561,1524.

EXAMPLE 16 1,3,5-Trimethyl-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1,3,5-trimethyl-4-pyrazolecarboxylic acid as starting materials, inrelative proportions similar to those used in that Example, the titlecompound was obtained as a white powder, melting at 75°-77° C., in a 69%yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.52 (2H,multiplet); 1.52-1.69 (4H, multiplet); 2.36 (3H, singlet); 2.30-2.49(4H, multiplet); 2.46 (3H, singlet); 3.44 (2H, singlet); 3.71 (3H,singlet); 4.19 (2H, triplet, J=6.1 Hz); 4.96 (2H, doublet, J=6.4 Hz);5.75-5.91 (3H, multiplet); 6.74 (1H, singlet); 6.89 (1H, doublet, J=4.9Hz); 8.00 (1H, doublet, J=4.9 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3344, 2930, 1617,1561, 1410.

EXAMPLE 17 3-Amino-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and3-amino-4-pyrazolecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as a white powder, melting at 172°-174° C., in a 38% yield.

Nuclear Magnetic Resonance Spectrum (hexadeuterated dimethyl sulfoxide),δ ppm: 1.32-1.45 (2H, multiplet); 1.45-1.57 (4H, multiplet); 2.26-2.44(4H, multiplet); 3.42 (2H, singlet); 3.92 (2H, triplet, J=5.9 Hz); 4.92(2H, doublet, J=5.9 Hz); 5.52-5.78 (2H, multiplet); 6.72 (1H, singlet);6.92 (1H, doublet, J=5.4 Hz); 7.67-7.79 (1H, broad); 7.88 (1H, broadtriplet, J=5.4 Hz); 8.08 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3229, 2934, 1616,1529, 1399.

EXAMPLE 18 N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-3-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and3-pyrazolecarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 57% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.52 (2H,multiplet); 1.52-1.65 (4H, multiplet); 2.31-2.50 (4H, multiplet); 3.43(2H, singlet); 4.21 (2H, triplet, J=6.3 Hz); 4.96 (2H, doublet, J=6.6Hz); 5.77-5.99 (2H, multiplet); 6.80-6.89 (3H, multiplet); 7.21-7.31(1H, broad); 7.57 (1H, doublet, J=2.0 Hz); 8.08 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2925, 1655, 1610,1560 (shoulder), 1540.

EXAMPLE 19 5-Methyl-N-[4-(piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-3-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and5-methyl-3-pyrazolecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as a white powder, melting at 93°-95° C., in a 52% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.52 (2H,multiplet); 1.52-1.66 (4H, multiplet); 2.33 (3H, singlet); 2.31-2.48(4H, multiplet); 3.42 (2H, singlet); 4.20 (2H, triplet, J=6.4 Hz); 4.96(2H, doublet, J=6.8 Hz); 5.72-5.81 (1H, multiplet); 5.83-5.93 (1H,multiplet); 6.55 (1H, singlet); 6.76 (1H, singlet); 6.87 (1H, doublet,J=5.4 Hz); 7.06-7.20 (1H, broad); 8.08 (1H, doublet, J=5.4 Hz);10.37-10.93 (1H, broad).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3195, 2931, 1645,1612, 1558.

EXAMPLE 20N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]furan-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and2-furancarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in an 82% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.35-1.53 (2H,multiplet); 1.53-1.80 (4H, multiplet); 2.25-2.60 (4H, multiplet); 3.48(2H, singlet); 4.22 (2H, triplet, J=6.4 Hz); 4.98 (2H, doublet, J=6.8Hz); 5.70-5.82 (1H, multiplet); 5.84-5.96 (1H, multiplet); 6.49 (1H,doublet of doublets, J=3.4 & 2.0 Hz); 6.58-6.72 (1H, multiplet); 6.77(1H, singlet); 6.85-7.03 (1H, multiplet); 7.11 (1H, doublet of doublets,J=3.4 & 1.0 Hz); 7.43 (1H, triplet, J=1.0 Hz); 8.10 (1H, doublet, J=5.3Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3430, 2930, 1655,1610, 1595, 1518, 1475, 1415, 1400, 1295, 1285.

EXAMPLE 21 5-Methyl-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]thiophene-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and5-methyl-2-thiophenecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compound,melting at 71°-73° C., was obtained in a yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.45-1.55 (2H,multiplet); 1.55-1.80 (4H, multiplet); 2.30-2.60 (4H, multiplet); 3.48(2H, singlet); 4.20 (2H, triplet, J=6.3 Hz); 4.97 (2H, doublet, J=6.3Hz); 5.78-5.82 (1H, multiplet); 5.82-5.93 (1H, multiplet); 6.20-6.35(1H, broad); 6.72 (1H, doublet, J=3.5 Hz); 6.78 (1H, singlet); 6.87-7.03(1H, multiplet); 7.31 (1H, doublet, J=3.5 Hz); 8.07 (1H, doublet, J=5.4Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3430, 2920, 1640,1505, 1415, 1400, 1295, 1285, 1032.

EXAMPLE 22 3-Amino-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]thiophene-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and3-amino-2-thiophenecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as colorless needles, melting at 138°-140° C., in a 40%yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.40-1.52 (2H,multiplet); 1.52-1.65 (4H, multiplet); 2.28-2.44 (4H, multiplet); 3.41(2H, singlet); 4.17 (2H, triplet, J=5.9 Hz); 4.96 (2H, doublet, J=5.9Hz); 5.60 (2H, broad singlet); 5.67-5.94 (3H, multiplet); 6.55 (1H,doublet, J=5.3 Hz); 6.74 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz);7.12 (1H, doublet, J=5.3 Hz); 8.08 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3300, 2935, 1617,1560, 1525, 1402, 1313, 1299, 1291.

EXAMPLE 23N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]thiophene-3-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and3-thiophenecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as an oil in a 90% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.52 (2H,multiplet); 1.52-1.65 (4H, multiplet); 2.30-2.45 (4H, multiplet); 3.41(1H, singlet); 4.22 (2H, triplet, J=6.1 Hz); 4.98 (2H, doublet, J=6.4Hz); 5.73-5.93 (2H, multiplet); 6.40-6.60 (1H, broad); 6.74 (1H,singlet); 6.87 (1H, doublet, J=5.4 Hz); 7.32 (1H, doublet of doublets,J=5.2 & 2.9 Hz); 7.39 (1H, doublet, J=5.2 Hz); 7.85 (1H, doublet, J=2.9Hz); 8.01 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2930, 1655(shoulder), 1645, 1610, 1560, 1535, 1500, 1415, 1400, 1285.

EXAMPLE 24 5-Chloro-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]thiophene-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and5-chloro-3-thiophenecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as colorless prisms, melting at 75°-77° C., in a 54% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.52 (2H,multiplet); 1.52-1.68 (4H, multiplet); 2.30-2.42 (4H, multiplet); 3.41(2H, singlet); 4.19 (2H, triplet, J=6.1 Hz); 4.97 (2H, doublet, J=6.8Hz); 5.70-5.84 (1H, multiplet); 5.84-5.95 (1H, multiplet); 6.41-6.53(1H, broad); 6.74 (1H, singlet); 6.88 (1H, doublet, J=5.4 Hz); 7.19 (1H,doublet, J=2.0 Hz); 7.62 (1H, doublet, J=2.0 Hz); 7.99 (1H, doublet,J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 2930, 1655,1610, 1415, 1400, 1298, 1285, 1032.

EXAMPLE 25 5-Phenyl-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]isoxazole-3-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and5-phenyl-3-isoxazolecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compound,melting at 105°-106° C., was obtained as colorless prisms in a 50%yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.51 (2H,multiplet); 1.51-1.67 (4H, multiplet); 2.29-2.46 (4H, multiplet); 3.43(2H, singlet); 4.27 (2H, triplet, J=6.3 Hz); 4.99 (2H, doublet, J=6.6Hz); 5.72-5.82 (1H, multiplet); 5.88-5.97 (1H, multiplet); 6.75 (1H,singlet); 6.91 (1H, doublet, J=5.4 Hz); 6.97 (1H, singlet); 7.13-7.27(1H, broad); 7.44-7.55 (3H, multiplet); 7.75-7.84 (2H, multiplet); 8.12(1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3322, 2936, 1668,1613, 1561, 1448.

EXAMPLE 26 N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]thiazole-4-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and4-thiazolecarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 68% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.52 (2H,multiplet); 1.52-1.67 (4H, multiplet); 2.24-2.53 (4H, multiplet); 3.43(2H, singlet); 4.26 (2H, triplet, J=6.4 Hz); 4.98 (2H, doublet, J=6.4Hz); 5.72-5.81 (1H, multiplet); 5.86-5.96 (1H, multiplet); 6.75 (1H,singlet); 6.90 (1H, doublet, J=5.4 Hz); 7.40-7.58 (1H, broad); 8.11 (1H,doublet, J=5.4 Hz); 8.18 (1H, doublet, J=2.4 Hz); 8.75 (1H, doublet,J=2.4 Hz).

Infrared Absorption Spectrum (liquid film), ν_(max) cm⁻¹ : 2936, 1664,1611, 1560, 1540, 1481, 1420, 1403, 1313, 1288.

EXAMPLE 27 N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-1,2,3-thiadiazole-4-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1,2,3-thiadiazole-4-carboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as colorless needles, melting at 70°-72° C., in a 52%yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.28-1.53 (2H,multiplet); 1.53-1.82 (4H, multiplet); 2.24-2.55 (4H, multiplet); 3.46(2H, singlet); 4.35 (2H, triplet, J=6.3 Hz); 5.01 (2H, doublet, J=6.3Hz); 5.75-5.87 (1H, multiplet); 5.87-6.00 (1H, multiplet); 6.77 (1H,singlet); 6.85-7.00 (1H, multiplet); 7.72-7.90 (1H, broad); 8.13 (1H,doublet, J=5.4 Hz); 9.23 (1H, singlet).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3425, 2940, 1675,1612, 1540, 1420, 1402, 1300, 1290, 1260, 1035.

EXAMPLE 28N-{4-[4-(1-Pyrrolidinylmethyl)-2-pyridyloxy]-cis-2-butenyl}pyrazole-4-carboxamide

Following a procedure similar to that described in Example 13, but using4-[4-(1-pyrrolidinylmethyl)-2-pyridyloxy]-cis-2-butenylamine and4-pyrazolecarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas a white powder, melting at 57°-61° C., in a 34% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.75-1.90 (4H,multiplet); 2.50-2.67 (4H, multiplet); 3.61 (2H, singlet); 4.17 (2H,triplet, J=5.9 Hz); 4.95 (2H, doublet, J=6.4 Hz); 5.69-5.92 (2H,multiplet); 6.72 (1H, broad triplet, J=5.4 Hz); 6.77 (1H, singlet); 6.90(1H, doublet, J=5.4 Hz); 7.96 (2H, singlet); 8.04 (1H, doublet, J=5.4Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 2962, 1626, 1610,1568, 1539, 1421, 1410, 1400.

EXAMPLE 29N-{4-[4-(1-Pyrrolidinylmethyl)-2-pyridyloxy]-cis-2-butenyl}pyrrole-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-[4-(1-pyrrolidinylmethyl)-2-pyridyloxy]-cis-2-butenylamine and2-pyrrolecarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas a white powder, melting at 124°-127° C., in a 64% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.71-1.88 (4H,multiplet); 2.43-2.61 (4H, multiplet); 3.57 (2H, singlet); 4.21 (2H,triplet, J=6.3 Hz); 4.97 (2H, doublet, J=6.6 Hz); 5.70-5.80 (1H,multiplet); 5.83-5.94 (1H, multiplet); 6.16-6.25 (1H, multiplet);6.30-6.42 (1H, broad); 6.53-6.59 (1H, multiplet); 6.88-6.96 (2H,multiplet); 8.07 (1H, doublet, J=5.3 Hz); 9.67-9.92 (1H, broad).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3252, 1637, 1617,1561, 1528, 1428, 1423, 1401, 1307, 1029.

EXAMPLE 30 4-Hydroxy-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]isoxazole-3-carboxamide

375 mg of ethyl 4-hydroxy-3-isoxazolecarboxylate (prepared as describedin Preparation 4) were added to a solution of 520 mg of4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine in 10 ml oftoluene, and the resulting mixture was heated under reflux for 6 hours.At the end of this time, the solvent was removed by distillation underreduced pressure, and the residue was dissolved in ethyl acetate. Theresulting solution was washed with a saturated aqueous solution ofsodium hydrogencarbonate and then with a saturated aqueous solution ofsodium chloride, after which it was dried over anhydrous magnesiumsulfate. The solvent was then removed by distillation under reducedpressure, and the residue was purified by column chromatography throughsilica gel, using a 1:19 by volume mixture of methanol and ethyl acetateas the eluent, to give 228 mg (yield 31%) of the title compound as anoil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.33-1.50 (2H,multiplet); 1.50-1.65 (4H, multiplet); 2.25-2.46 (4H, multiplet); 3.42(2H, singlet); 4.26 (2H, triplet, J=6.6 Hz); 4.98 (2H, doublet, J=6.6Hz); 5.67-5.82 (1H, multiplet); 5.88-6.00 (1H, multiplet); 6.75 (1H,singlet); 6.90 (1H, doublet, J=5.3 Hz); 7.25-7.42 (1H, broad); 8.13 (1H,doublet, J=5.3 Hz); 8.22 (1H, singlet).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2930, 1680, 1610,1560 (shoulder), 1550.

EXAMPLE 31 1-Methyl-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrrole-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1-methyl-2-pyrrolecarboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as an oil in a 76% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.51 (2H,multiplet); 1.51-1.65 (4H, multiplet); 2.33-2.43 (4H, multiplet); 3.42(2H, singlet); 3.94 (3H, singlet); 4.16 (2H, triplet, J=6.1 Hz); 4.97(2H, doublet, J=6.8 Hz); 5.71-5.83 (1H, multiplet); 5.83-5.94 (1H,multiplet); 6.06 (1H, doublet of doublets, J=3.9 & 2.2 Hz); 6.14-6.24(1H, broad); 6.53 (1H, doublet of doublets, J=7.8 & 2.2 Hz); 6.69-6.73(1H, multiplet); 6.74 (1H, singlet); 6.89 (1H, doublet, J=5.2 Hz); 8.04(1H, doublet, J=5.2 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2935, 1655(shoulder), 1645, 1610, 1560, 1535, 1500, 1475, 1415, 1400.

The hydrochloride of the title compound, melting at 136°-137° C., wasprepared by dissolving the title compound, obtained as described above,in ethyl acetate, after which an ethyl acetate solution containing anequimolar amount of hydrogen chloride was added to the resultingsolution.

EXAMPLE 32 N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrrole-3-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and3-pyrrolecarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 74% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.33-1.51 (2H,multiplet); 1.51-1.67 (4H, multiplet); 2.27-2.49 (4H, multiplet); 3.41(2H, singlet); 4.18 (2H, triplet, J=6.3 Hz); 4.96 (2H, doublet, J=5.9Hz); 5.69-5.94 (2H, multiplet); 6.17-6.33 (1H, broad); 6.42 (1H, broadsinglet); 6.73 (2H, broad singlet); 6.87 (1H, doublet, J=4.9 Hz); 7.33(1H, broad singlet); 8.05 (1H, doublet, J=4.9 Hz); 9.31-9.54 (1H,broad).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3470, 2930, 1635,1610, 1560, 1510, 1415, 1400, 1310, 1295.

EXAMPLE 33 N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-pyrimidinylthio)acetamide

163 mg of 2-mercaptopyrimidine were added to a solution of 116 mg of 85%potassium hydroxide and 484 mg ofN-[4-(4-piperidinomethyl-2-pyridyl-cis-2-butenyl]-2-chloroacetamide(prepared as described in Preparation 1) in 10 ml of methanol, and theresulting mixture was stirred at room temperature for 7 hours. At theend of this time, the reaction mixture was concentrated by evaporationunder reduced pressure, and the concentrate was mixed with water, afterwhich it was extracted with ethyl acetate. The extract was freed fromthe solvent by distillation under reduced pressure. The residue thusobtained was recrystallized from ethyl acetate, to give 474 mg (yield80%) of the title compound as a white powder, melting at 103°-106° C.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.52-1.64 (4H, multiplet); 2.30-2.43 (4H, multiplet); 3.40(2H, singlet); 3.82 (2H, singlet); 4.29 (2H, triplet, J=6.3 Hz); 4.87(2H, doublet, J=5.9 Hz); 5.52-5.65 (1H, multiplet); 5.75-5.86 (1H,multiplet); 6.70 (1H, singlet); 6.87 (1H, doublet, J=5.4 Hz); 7.00-7.11(1H, broad); 7.02 (1H, doublet, J=4.9 Hz); 8.03 (1H, doublet, J=5.4 Hz);8.53 (2H, doublet, J=4.9 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3333, 2940, 2920,1643, 1560, 1552, 1524, 1397, 1316.

EXAMPLE 34 N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyrimidinylthio) butyramide

2.78 g of 2-mercaptopyrimidine were added to a solution of 1.95 g of 85%potassium hydroxide and 9.03 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide(prepared as described in Preparation 2) in 140 ml of methanol, and theresulting mixture was heated under reflux for 15 hours. At the end ofthis time, the reaction mixture was cooled, and the solvent was removedby distillation under reduced pressure. The resulting residue was mixedwith water, and the aqueous mixture was extracted with ethyl acetate.The extract was concentrated by evaporation under reduced pressure, andthe concentrate was purified by column chromatography through silicagel, using a 9:1 by volume mixture of ethyl acetate and methanol as theeluent, to give 10.1 g (yield 92%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.50 (2H,multiplet); 1.53-1.67 (4H, multiplet); 2.11 (2H, quintet, J=7.2 Hz);2.30-2.49 (6H, multiplet); 3.20 (2H, triplet, J=7.2 Hz); 3.41 (2H,singlet); 4.06 (2H, doublet, J=5.9 Hz); 4.93 (2H, doublet, J=6.3 Hz);5.64-5.73 (1H, multiplet); 5.80-5.89 (1H, multiplet); 6.27-6.41 (1H,broad); 6.73 (1H, singlet); 6.88 (1H, doublet, J=5.1 Hz); 6.94 (1H,triplet, J=4.9 Hz); 8.03 (1H, doublet, J=5.1 Hz); 8.49 (2H, doublet,J=4.9 Hz).

Infrared Absorption Spectrum (liquid film), ν_(max) cm⁻¹ : 3295, 2936,1646, 1611, 1564, 1548, 1420, 1403, 1382, 1312, 1300, 1289.

The compound obtained as described above was dissolved in ethyl acetate,and an ethyl acetate solution containing an equimolar amount of hydrogenchloride was added to the resulting solution. The mixture was stirred atroom temperature for 10 minutes, and then the solvent was removed bydistillation under reduced pressure, to give the hydrochloride of thetitle compound, melting at 123°-125° C.

EXAMPLE 35N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(4-methyl-2-pyrimidinylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 2-mercapto-4-methylpyrimidine as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as an oil in a 70% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.40-1.56 (2H,multiplet); 1.60-1.81 (4H, multiplet); 2.10 (2H, quintet, J=7.1 Hz);2.39 (2H, triplet, J=7.1 Hz); 2.44 (3H, singlet); 2.35-2.70 (4H,multiplet); 3.20 (2H, triplet, J=7.1 Hz); 3.55 (2H, singlet); 4.05 (2H,triplet, J=6.1 Hz); 4.93 (2H, doublet, J=6.3 Hz); 5.64-5.73 (1H,multiplet); 5.78-5.87 (1H, multiplet); 6.25-6.37 (1H, broad); 6.76-6.81(2H, multiplet); 6.98 (1H, singlet); 8.08 (1H, triplet, J=5.4 Hz); 8.34(1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2930, 1660, 1610,1570, 1560, 1540, 1415, 1325.

EXAMPLE 36N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(1-methylimidazol-2-ylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 2-mercapto-1-methylimidazole as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as an oil in a 49% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.50 (2H,multiplet); 1.50-1.62 (4H, multiplet); 2.03 (2H, quintet, J=6.8 Hz);2.30-2.46 (6H, multiplet); 3.08 (2H, triplet, J=6.8 Hz); 3.41 (2H,singlet); 3.60 (3H, singlet); 4.04 (2H, triplet, J=6.1 Hz); 4.93 (2H,doublet, J=5.9 Hz); 5.63-5.73 (1H, multiplet); 5.76-5.91 (1H,multiplet); 6.72 (1H, singlet); 6.89 (1H, doublet, J=5.4 Hz); 6.90 (1H,singlet); 7.01 (1H, singlet); 7.24-7.38 (1H, broad); 8.04 (1H, doublet,J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3250, 2940, 1660,1610, 1560, 1420, 1290.

EXAMPLE 37N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(5-methyl-1,3,4-oxadiazol-2-ylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 2-mercapto-5-methyl -1,3,4-oxadiazole as starting materials, inrelative proportions similar to those used in that Example, the titlecompound was obtained as an oil in a 79% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.50-1.65 (4H, multiplet); 2.17 (2H, quintet, J=7.3 Hz);2.31-2.41 (6H, multiplet); 2.51 (3H, singlet); 3.28 (2H, triplet, J=7.3Hz); 3.41 (2H, singlet); 4.04 (2H, triplet, J=5.9 Hz); 4.93 (2H,doublet, J=6.6 Hz); 5.64-5.75 (1H, multiplet); 5.79-5.90 (1H,multiplet); 6.39-6.54 (1H, broad); 6.73 (1H, singlet); 6.89 (1H,doublet, J=5.3 Hz); 8.04 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3440, 2930, 1660,1610, 1560, 1510, 1480, 1420.

EXAMPLE 38N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(1,3,4-thiadiazol-2-ylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 2-mercapto-1,3,4-thiadiazole as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as an oil in an 84% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.51 (2H,multiplet); 1.51-1.68 (4H, multiplet); 2.20 (2H, quintet, J=7.3 Hz);2.27-2.45 (6H, multiplet); 3.41 (2H, singlet); 3.43 (2H, triplet, J=7.3Hz); 5.63-5.73 (1H, multiplet); 5.78-5.89 (1H, multiplet); 6.34-6.51(1H, broad); 6.73 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.04 (1H,doublet, J=5.3 Hz); 9.00 (1H, singlet).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3350, 3300, 2940,1660, 1610, 1560, 1510, 1420.

EXAMPLE 39N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(5-methyl-1,3,4-thiadiazol-2-ylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 2-mercapto-5-methyl -1,3,4-thiadiazole as starting materials, inrelative proportions similar to those used in that Example, the titlecompound was obtained as a white powder, melting at 65°-68° C., in a 78%yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.51 (2H,multiplet); 1.51-1.68 (4H, multiplet); 2.16 (2H, quintet, J=6.9 Hz);2.31-2.44 (6H, multiplet); 2.71 (3H, singlet); 3.35 (2H, triplet, J=6.9Hz); 3.41 (2H, singlet); 4.04 (2H, triplet, J=5.9 Hz); 4.94 (2H,doublet, J=6.6 Hz); 5.65-5.76 (1H, multiplet); 5.77-5.90 (1H,multiplet); 6.37-6.50 (1H, broad); 6.73 (1H, singlet); 6.89 (1H,doublet, J=5.3 Hz); 8.04 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 3300, 2940,1660, 1610, 1560, 1510, 1420, 1300.

EXAMPLE 40N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(1,2,4-triazol-3-ylthio)acetamide

Following a procedure similar to that described in Example 33, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenyl]-2-chloroacetamide(prepared as described in Preparation 1) and 3-mercapto-1,2,4-triazoleas starting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as a white powder, meltingat 65°-67° C., in a 91% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.41-1.55 (2H,multiplet); 1.55-1.67 (4H, multiplet); 2.42-2.55 (4H, multiplet); 3.47(2H, singlet); 3.77 (2H, singlet); 4.00 (2H, triplet, J=6.3 Hz); 4.83(2H, doublet, J=6.8 Hz); 5.71-5.80 (1H, multiplet); 5.85-5.94 (1H,multiplet); 6.73 (1H, singlet); 6.85 (1H, doublet, J=5.1 Hz); 7.32-7.44(1H, broad); 8.06 (1H, doublet, J=5.1 Hz); 8.07 (1H, singlet).

Infrared Absorption Spectrum (liquid film), ν_(max) cm⁻¹ : 2935, 1652,1612, 1560, 1421, 1403, 1301, 1288.

EXAMPLE 41N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(1,2,4-triazol-3-ylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 3-mercapto-1,2,4-triazole as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as a white powder, melting at 87°-89° C., in a 56% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.51 (2H,multiplet); 1.54-1.65 (4H, multiplet); 2.09 (2H, quintet, J=7.0 Hz);2.33-2.50 (6H, multiplet); 3.13 (2H, triplet, J=7.0 Hz); 3.44 (2H,singlet); 4.06 (2H, triplet, J=6.1 Hz); 4.93 (2H, doublet, J=6.4 Hz);5.69-5.82 (1H, multiplet); 5.82-5.9 3 (1H, multiplet); 6.75 (1H,singlet); 6.89 (1H, doublet, J=5.4 Hz); 6.92-7.0 3 (1H, broad); 8.03(1H, singlet); 8.04 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 2942, 2915, 1625,1614, 1564, 1293, 1250, 1238.

EXAMPLE 42N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(1-methyltetrazol-5-ylthio)acetamide

Following a procedure similar to that described in Example 33, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenyl]-2-chloroacetamide(prepared as described in Preparation 1) and1-methyl-5-mercaptotetrazole as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as a white powder, melting at 58°-62° C., in an 87% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.35-1.50 (2H,multiplet); 1.50-1.63 (4H, multiplet); 2.27-2.44 (4H, multiplet); 3.41(2H, singlet); 3.95 (3H, singlet); 3.96 (2H, singlet); 4.04 (2H,triplet, J=5.9 Hz); 4.90 (2H, doublet, J=5.9 Hz); 5.54-5.68 (1H,multiplet); 5.78-5.89 (1H, multiplet); 6.73 (1H, singlet); 6.88 (1H,doublet, J=5.9 Hz); 8.05 (1H, doublet, J=5.9 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3300, 2950, 1730,1670, 1610, 1560, 1400, 1290.

EXAMPLE 43N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(1-methyltetrazol-5-ylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 1-methyl-5-mercaptotetrazole as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as an oil in a 70% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.50 (2H,multiplet); 1.50-1.63 (4H, multiplet); 2.13-2.24 (2H, quintet, J=7.3Hz); 2.26-2.47 (6H, multiplet); 3.40 (2H, triplet, J=7.3 Hz); 3.41 (2H,singlet); 3.91 (3H, singlet); 4.05 (2H, triplet, J=5.3 Hz); 4.94 (2H,doublet, J=6.6 Hz); 5.66-5.75 (1H, multiplet); 5.80-5.89 (1H,multiplet); 6.39-6.50 (1H, broad); 6.73 (1H, singlet); 6.89 (1H,doublet, J=5.2 Hz); 8.03 (1H, doublet, J=5.2 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 2925, 1660,1610, 1560, 1510, 1410, 1290.

EXAMPLE 44N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-[1-(2-hydroxyethyl)tetrazol-5-ylthio]butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 1-(2-hydroxyethyl)-5-mercaptotetrazole as starting materials, inrelative proportions similar to those used in that Example, the titlecompound was obtained as an oil in a 63% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.50 (2H,multiplet); 1.50-1.63 (4H, multiplet); 2.17 (2H, quintet, J=6.8 Hz);2.33-2.60 (6H, multiplet); 3.38 (2H, triplet, J=6.8 Hz); 3.49 (2H,singlet); 4.01 (2H, triplet, J=6.1 Hz); 4.08-4.11 (2H, multiplet);4.34-4.38 (2H, multiplet); 4.92 (2H, doublet, J=6.4 Hz); 5.67-5.87 (2H,multiplet); 6.49-6.65 (1H, broad); 6.79 (1H, singlet); 6.93 (1H,doublet, J=4.9 Hz); 8.05 (1H, doublet, J=4.9 Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3300, 2940, 1660,1610, 1560, 1510, 1420, 1400.

EXAMPLE 45N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyridylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 2-mercaptopyridine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 53% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.40-1.53 (2H,multiplet); 1.59-1.75 (4H, multiplet); 2.07 (2H, quintet, J=7.1 Hz);2.39 (2H, triplet, J=7.1 Hz); 2.33-2.60 (4H, broad); 3.21 (2H, triplet,J=7.1 Hz); 3.51 (2H, singlet); 4.07 (2H, triplet, J=6.2 Hz); 4.94 (2H,doublet, J=6.3 Hz); 5.63-5.75 (1H, multiplet); 5.80-5.88 (1H,multiplet); 6.58-6.69 (1H, broad); 6.77 (1H, singlet); 6.92-7.00 (2H,multiplet); 7.17 (1H, triplet of doublets, J=8.3 & 1.0 Hz); 7.46 (1H,doublet of triplets, J=8.3 & 2.0 Hz); 8.07 (1H, doublet, J=5.4 Hz); 8.39(1H, triplet of doublets, J=4.9 & 1.0 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2945, 1660, 1655(shoulder), 1610, 1580, 1560, 1415.

EXAMPLE 46N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(4-pyridylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 4-mercaptopyridine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 33% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.48 (2H,multiplet); 1.54-1.63 (4H, multiplet); 2.07 (2H, quintet, J=7.2 Hz);2.25-2.3 9 (6H, multiplet); 3.05 (2H, triplet, J=7.2 Hz); 3.41 (2H,singlet); 4.04 (2H, triplet, J=5.9 Hz); 4.92 (2H, doublet, J=6.6 Hz);5.63-5.75 (1H, multiplet); 5.78-5.96 (1H, multiplet); 6.15-6.27 (1H,broad); 6.73 (1H, singlet); 6.88 (1H, doublet, J=5.3 Hz); 7.13 (2H,doublet, J=4.6 Hz); 8.02 (1H, doublet, J=5.3 Hz); 8.37 (2H, doublet,J=4.6 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 2945, 1660, 1655(shoulder), 1610, 1580, 1560, 1415, 1405, 1310, 1300, 1290.

EXAMPLE 47N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(4,6-diamino-2-pyrimidinylthio)butyramide

Following a procedure similar to that described in Example 34, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide (prepared as described in Preparation2) and 4,6-diamino-2-mercaptopyrimidine as starting materials, inrelative proportions similar to those used in that Example, the titlecompound was obtained as an oil in a 48% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.50 (2H,multiplet); 1.55-1.67 (4H, multiplet); 1.83-2.14 (4H, multiplet);2.30-2.47 (6H, multiplet); 3.10 (2H, triplet, J=6.8 Hz); 3.45 (2H,singlet); 3.99-4.09 (2H, multiplet); 4.61 (2H, broad singlet); 4.92 (2H,doublet, J=6.8 Hz); 5.24 (1H, singlet); 5.63-5.72 (1H, multiplet);5.78-5.87 (1H, multiplet); 6.12-6.23 (1H, broad); 6.72-6.79 (1H,multiplet); 6.91 (1H, doublet, J=4.4 Hz); 8.05 (1H, doublet, J=4.4 Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 2940, 1655, 1610,1580, 1555, 1310.

EXAMPLE 48 N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-N'-isopropylurea

A solution of 0.113 g of isopropylamine in 2 ml of methylene chloridewas added to a solution of 0.31 g of carbonyldiimidazole in 5 ml ofmethylene chloride, and the resulting mixture was cooled with ice, afterwhich a solution of 0.500 g of 4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine in 5 ml of methylene chloride was added. Thereaction mixture was stirred at room temperature for 2 hours, afterwhich it was poured into ice-water and extracted with methylenechloride. The extract was dried over anhydrous magnesium sulfate, andthe solvent was removed by distillation under reduced pressure. Theresidue was purified by column chromatography through silica gel, usinga 1:20 by volume mixture of methanol and ethyl acetate as the eluent, togive 0.41 g (yield 62%) of the title compound as a white powder, meltingat 90°-92° C.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.13 (6H, doublet,J=6.4 Hz); 1.40-1.55 (2H, multiplet); 1.55-1.90 (6H, multiplet);2.30-2.57 (4H, multiplet); 3.49 (2H, singlet); 3.80-3.90 (1H,multiplet); 3.95 (2H, triplet, J=5.9 Hz); 4.10-4.30 (1H, broad);4.52-4.67 (1H, broad); 4.91 (2H, doublet, J=6.3 Hz); 5.67-5.88 (2H,multiplet); 6.80 (1H, singlet); 6.92 (1H, doublet, J=5.9 Hz); 8.07 (1H,doublet, J=5.9 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3430, 2920, 1655,1605, 1555, 1520, 1410.

EXAMPLE 49 N-Diphenylmethyl-N'-[4-(47piperidinomethyl)-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine anddiphenylmethylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 69% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.42 (2H,multiplet); 1.42-1.70 (4H, multiplet); 2.28-2.57 (4H, multiplet); 3.44(2H, singlet); 3.94 (2H, triplet, J=5.9 Hz); 4.86 (2H, doublet, J=6.3Hz); 4.87 (1H, singlet); 5.10-5.24 (1H, broad); 5.58-5.70 (1H,multiplet); 5.72-5.83 (1H, multiplet); 5.97 (1H, doublet, J=7.3 Hz);6.74 (1H, singlet); 6.87 (1H, doublet, J=5.4 Hz); 7.13-7.42 (10H,multiplet); 8.00 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃ .sup.), ν_(max) cm⁻¹ : 3430, 2980,2930, 1660, 1610, 1560, 1520, 1415, 1400, 1298, 1285.

EXAMPLE 50 N-(1-Methylpropyl)-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1-methylpropylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas a white powder, melting at 72°-74° C., in an 80% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 0.90 (3H, triplet,J=7.5 Hz); 1.11 (3H, doublet, J=6.4 Hz); 1.35-1.80 (6H, multiplet);2.33-2.60 (4H, multiplet); 3.51 (2H, singlet); 3.60-3.77 (1H,multiplet); 3.95 (2H, triplet, J=5.9 Hz); 4.13-4.28 (1H, broad);4.54-4.69 (1H, broad); 4.92 (2H, doublet, J=6.5 Hz); 6.67-6.88 (2H,multiplet); 6.81 (1H, singlet); 6.93 (1H, doublet, J=5.4 Hz); 8.07 (1H,doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3430, 3350, 2920,1655, 1610, 1558, 1525, 1415, 1400, 1340, 1298, 1285.

EXAMPLE 51 N-(1-Methylbutyl)-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1-methylbutylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 66% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 0.89 (3H, triplet,J=7.1 Hz); 1.10 (3H, doublet, J=6.4 Hz); 1.22-1.50 (6H, multiplet);1.50-1.64 (4H, multiplet); 2.30-2.43 (4H, multiplet); 3.41 (2H,singlet); 3.67-3.82 (1H, multiplet); 3.95 (2H, triplet, J=5.9 Hz); 4.17(1H, broad doublet, J=7.8 Hz); 4.58-4.68 (1H, broad); 4.91 (2H, doublet,J=6.8 Hz); 5.66-5.76 (1H, multiplet); 5.76-5.88 (1H, multiplet); 6.73(1H, singlet); 6.80 (1H, doublet, J=5.9 Hz); 8.04 (1H, doublet, J=5.9Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3430, 3350, 2930,1650, 1610, 1558, 1525, 1415, 1400, 1310, 1295, 1285.

EXAMPLE 52 N-(1-Methylhexyl)-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1-methylhexylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 65% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 0.87 (3H, triplet,J=6.6 Hz); 1.10 (3H, doublet, J=6.4 Hz); 1.20-1.50 (10H, multiplet);1.50-1.67 (4H, multiplet); 2.30-2.47 (4H, multiplet); 3.42 (2H,singlet); 3.64-3.80 (1H, multiplet); 3.95 (2H, triplet, J=6.1 Hz);4.07-4.20 (1H, broad doublet, J=7.7 Hz); 4.25-4.65 (1H, broad); 4.92(2H, doublet, J=6.3 Hz); 5.63-5.88 (2H, multiplet); 6.74 (1H, singlet);6.89 (1H, doublet, J=5.3 Hz); 8.05 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3430, 3350, 2930,2850, 1655, 1610, 1560, 1528, 1415, 1400, 1310, 1298, 1285.

EXAMPLE 53 N-(1-Phenylethyl)-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1-phenylethylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 62% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.45 (3H, doublet,J=6.8 Hz); 1.50-1.74 (6H, multiplet); 2.30-2.43 (4H, multiplet); 3.41(2H, singlet); 3.92 (2H, triplet, J=5.6 Hz); 4.50-4.70 (2H, broad); 4.86(2H, doublet, J=6.3 Hz); 5.57-5.68 (1H, multiplet); 5.72-5.84 (1H,multiplet); 6.71 (1H, singlet); 6.86 (2H, doublet, J=5.4 Hz); 7.19-7.37(5H, multiplet); 8.01 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ : 3440, 2980, 2930,1660, 1610, 1558, 1525, 1415, 1400, 1298, 1285.

EXAMPLE 54 N-(1-Ethylpropyl)-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1-ethylpropylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas a white powder, melting at 82°-84° C., in a 77% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 0.89 (6H, triplet,J=7.3 Hz); 1.22-1.78 (10H, multiplet); 2.30-2.56 (4H, multiplet); 3.49(2H, singlet); 3.96 (2H, triplet, J=6.1 Hz); 4.05-4.20 (1H, broad);4.57-4.68 (1H, broad); 4.92 (2H, doublet, J=6.3 Hz); 5.65-5.88 (2H,multiplet); 6.80 (1H, singlet); 6.92 (1H, doublet, J=5.3 Hz); 8.07 (1H,doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3440, 3370, 2960,2930, 1655, 1622, 1540, 1528, 1418, 1400, 1300, 1285.

EXAMPLE 55N-(1,2-Dimethylpropyl)-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1,2-dimethylpropylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 73% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 0.87 (3H, triplet,J=6.8 Hz); 0.88 (3H, doublet, J=6.8 Hz); 1.05 (3H, doublet, J=5.8 Hz);1.37-1.51 (2H, multiplet); 1.51-1.82 (5H, multiplet); 2.30-2.42 (4H,multiplet); 3.56 (2H, singlet); 3.56-3.71 (1H, multiplet); 3.95 (2H,triplet, J=6.1 Hz); 4.20 (1H, broad doublet, J=8.8 Hz); 4.58-4.70 (1H,broad); 4.92 (2H, doublet, J=6.3 Hz); 5.65-5.77 (1H, multiplet);5.77-5.88 (1H, multiplet); 6.73 (1H, sin91et); 6.88 (1H, doublet, J=5.4Hz); 8.04 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3440, 2930, 1660,1610, 1560, 1525, 1415, 1400, 1308, 1300, 1285.

EXAMPLE 56 N-(1,2-Diphenylethyl)-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine and1,2-diphenylethylamine as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in an 80% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.54 (2H,multiplet); 1.54-1.84 (4H, multiplet); 2.32-2.62 (4H, multiplet); 3.05(2H, doublet, J=6.8 Hz); 3.52 (2H, singlet); 3.85 (2H, triplet, J=5.9Hz); 4.63-4.78 (1H, broad); 4.83 (2H, doublet, J=6.8 Hz); 4.90-5.02 (1H,multiplet); 5.52-5.62 (1H, multiplet); 5.68-5.79 (1H, multiplet);6.74-6.87 (1H, broad); 6.91 (1H, doublet, J=5.3 Hz); 7.00-7.08 (2H,multiplet); 7.12-7.39 (8H, multiplet); 8.02 (1H, doublet, J=5.3 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 3010, 2950,1668, 1615, 1560, 1528, 1420, 1408, 1300, 1290.

EXAMPLE 57 N-Cyclopropyl-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine andcyclopropylamine as starting materials, in relative proportions similarto those used in that Example, the title compound was obtained as awhite powder, melting at 102°-104° C., in a 60% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.51-1.59 (2H,multiplet); 1.67-1.77 (2H, multiplet); 1.36-1.82 (6H, multiplet);2.30-2.60 (4H, multiplet); 3.49 (2H, singlet); 4.04 (2H, triplet, J=6.1Hz); 4.62-4.78 (1H, broad); 4.94 (2H, doublet, J=6.4 Hz); 5.02-5.17 (1H,broad); 5.67-5.90 (2H, multiplet); 6.78 (1H, singlet); 6.93 (1H,doublet, J=5.4 Hz); 8.07 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3430, 2990, 2930,1642, 1610, 1560, 1528, 1415, 1400, 1298, 1285.

EXAMPLE 58 N-Cyclobutyl-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine andcyclobutylamine as starting materials, in relative proportions similarto those used in that Example, the title compound was obtained as awhite powder, melting at 130°-132° C., in a 66% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.49 (2H,multiplet); 1.52-1.88 (8H, multiplet); 2.23-2.42 (6H, multiplet); 3.41(2H, singlet); 3.95 (2H, triplet, J=5.8 Hz); 4.03-4.21 (1H, multiplet);4.50-4.68 (2H, multiplet); 4.91 (2H, doublet, J=6.4 Hz); 5.62-5.74 (1H,multiplet); 5.76-5.89 (1H, multiplet); 6.74 (1H, singlet); 6.88 (1H,doublet, J=5.4 Hz); 8.05 (1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3440, 2980, 2940,1660, 1612, 1560, 1528, 1415, 1400, 1300, 1288, 1248.

EXAMPLE 59 N-Cyclopentyl-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy) -cis-2-butenylamine andcyclopentylamine as starting materials, in relative proportions similarto those used in that Example, the title compound was obtained as awhite powder, melting at 121°-124° C., in a 77% yield.

Nuclear Magnetic Resonance Spectrum (hexadeuterated dimethyl sulfoxide),δ ppm: 1.14-1.67 (12H, multiplet); 1.67-1.82 (2H, multiplet); 2.20-2.43(4H, multiplet); 3.45 (2H, singlet); 3.72 (2H, triplet, J=5.8 Hz);3.75-3.91 (1H, multiplet); 4.86 (2H, doublet, J=6.4 Hz); 5.49-5.72 (2H,multiplet); 5.77 (1H, triplet, J=5.9 Hz); 5.84 (2H, doublet, J=7.3 Hz);6.71 (1H, singlet); 6.92 (1H, doublet of doublets, J=5.4 & 1.0 Hz); 8.07(1H, doublet, J=5.4 Hz).

Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3318, 2935, 1618,1584, 1561, 1426, 1409, 1301, 1041.

EXAMPLE 60 N-Cyclohexyl -N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine andcyclohexylamine as starting materials, in relative proportions similarto those used in that Example, the title compound was obtained as awhite powder, melting at 131°-132° C., in a 72% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃) δ ppm: 0.99-1.21 (2H,multiplet); 1.25-1.50 (4H, multiplet); 1.52-1.75 (8H, multiplet);1.85-1.97 (2H, multiplet); 2.30-2.42 (4H, multiplet); 3.40 (2H,singlet); 3.42-3.58 (1H, multiplet); 3.95 (2H, triplet, J=5.8 Hz); 4.25(1H, broad doublet, J=7.8 Hz); 4.61 (1H, broad triplet, J=5.9 Hz); 4.92(2H, doublet, J=6.8 Hz); 5.64-5.76 (1H, multiplet); 5.76-5.87 (1H,multiplet); 6.73 (1H, singlet); 6.87 (1H, doublet, J=5.4 Hz); 8.04 (1H,doublet, J=5.4 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3430, 3350, 2980, 2920, 2850, 1655, 1610, 1558, 1528, 1415, 1400, 1310,1300, 1288.

EXAMPLE 61N-Cycloheptyl-N'-[4-(4-iperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine andcycloheptylamine as starting materials, in relative proportions similarto those used in that Example, the title compound was obtained as awhite powder, melting at 89°-91° C., in a 60% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.32-1.80 (16H,multiplet); 1.82-2.00 (2H, multiplet); 2.25-2.50 (4H, multiplet); 3.43(2H, singlet); 3.64-3.80 (1H, multiplet); 3.95 (2H, triplet, J=5.9 Hz);4.29 (1H, broad doublet, J=7.3 Hz); 4.56 (1H, broad triplet, J=5.4 Hz);4.92 (2H, doublet, J=6.3 Hz); 5.64-5.77 (1H, multiplet); 5.77-5.88 (1H,multiplet); 6.75 (1H, singlet); 6.88 (1H, doublet, J=5.4 Hz); 8.05 (1H,doublet, J=5.4 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3430, 2920, 1655, 1610, 1558, 1520, 1413, 1400, 1308, 1298, 1285.

EXAMPLE 62N-Cyclooctyl-N'-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]urea

Following a procedure similar to that described in Example 48, but using4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine andcyclooctylamine as starting materials, in relative proportions similarto those used in that Example, the title compound was obtained as an oilin a 59% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.32-1.93 (20H,multiplet); 2.30-2.70 (4H, multiplet); 3.49 (2H, singlet); 3.68-3.86(1H, multiplet); 3.94 (2H, triplet, J=5.9 Hz); 4.27-4.43 (1H, broad);4.52-4.67 (1H, broad); 4.91 (2H, doublet, J=6.3 Hz); 5.65-5.88 (2H,multiplet); 6.80 (1H, singlet); 6.92 (1H, doublet, J=5.3 Hz); 8.07 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ :3440, 2930, 1655, 1610, 1560, 1525, 1415, 1400, 1310, 1300, 1288.

EXAMPLE 63N-Isopropyl-N'-[3-(4-piperidinomethyl-2-pyridyloxy)propyl]urea

Following a procedure similar to that described in Example 48, but using3-(4-piperidinomethyl-2-pyridyloxy)propylamine and isopropylamine asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as a white powder, meltingat 58°-60° C., in a 50% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.14 (6H, doublet,J=6.3 Hz); 1.38-1.50 (2H, multiplet); 1.52-1.64 (4H, multiplet);1.90-2.05 (2H, multiplet); 2.37 (4H, triplet, J=5.1 Hz); 3.34 (2H,triplet of doublets, J=6.3 & 5.8 Hz); 3.41 (2H, singlet); 3.74-3.92 (1H,multiplet); 4.19 (1H, broad doublet, J=7.8 Hz); 4.38 (2H, triplet, J=5.8Hz); 4.70-4.82 (1H, broad); 6.72 (1H, singlet); 6.86 (1H, doublet, J=5.4Hz); 8.04 (1H, doublet, J=5.4 Hz). Infrared Absorption Spectrum (CHCl₃),ν_(max) cm⁻¹ : 3420, 3320, 2920, 1650, 1608, 1555, 1530, 1412.

EXAMPLE 64N-[3-(4-Piperidinomethyl-2-pyridyloxy)propyl]-pyrazole-4-carboxamide

A solution of 1.0 g of 3-(4-piperidinomethyl-2-pyridyloxy)propylamineand 0.45 g of 4-pyrazolecarboxylic acid dissolved in 15 ml ofdimethylformamide was stirred for 5 minutes, whilst ice-cooling, afterwhich 734 mg of diethyl cyanophosphonate and 0.68 ml of triethylaminewere added to the resulting mixture. The mixture was then stirred atroom temperature for 3 hours, after which it was diluted with water, andthe aqueous mixture was extracted with ethyl acetate. The extract waswashed with a saturated aqueous solution of sodium hydrogencarbonate andthen with a saturated aqueous solution of sodium chloride, and driedover anhydrous magnesium sulfate. The solvent was then removed bydistillation under reduced pressure, and the resulting residue waspurified by column chromatography through silica gel, using a 1:9 byvolume mixture of methanol and chloroform as the eluent, to give 1.2 g(yield 85%) of the title compound as a white powder, melting at117°-119° C.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.47 (2H,multiplet); 1.50-1.62 (4H, multiplet); 1.99-2.11 (2H, multiplet);2.34-2.44 (4H, multiplet); 3.41 (2H, singlet); 3.55 (2H, quartet, J=5.9Hz); 4.42 (2H, triplet, J=5.9 Hz); 6.72 (1H, singlet); 6.88 (1H,doublet, J=5.3 Hz); 7.16 (2H, broad triplet, J=5.9 Hz); 7.99-8.05 (2H,multiplet); 8.05 (1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum(KBr), ν_(max) cm⁻¹ : 3250, 2935, 1631, 1607, 1566, 1421, 1386, 1302,1212.

EXAMPLE 65N-[4-(4-Piperidinomethyl-2-pyridyloxy)butyl]-pyrazole-4-carboxamide

Following a procedure similar to that described in Example 64, but using4-(4-piperidinomethyl-2-pyridyloxy)butylamine and 4-pyrazolecarboxylicacid as starting materials, in relative proportions similar to thoseused in that Example, the title compound was obtained as a white powder,melting at 145°-147° C., in a 71% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm. 1.39-1.50 (2H,multiplet); 1.53-1.62 (4H, multiplet); 1.71-1.92 (4H, multiplet);2.31-2.42 (4H, multiplet); 3.41 (2H, singlet); 3.49 (2H, doublet ofdoublets, J=12.5 & 6.6 Hz); 4.29 (2H, doublet of doublets, J=11.2 & 6.1Hz); 6.36-6.42 (1H, broad); 6.71 (1H, singlet); 6.85 (1H, doublet, J=5.3Hz); 7.96 (2H, singlet); 8.05 (1H, doublet, J=5.3 Hz). InfraredAbsorption Spectrum (KBr), ν_(max) cm⁻¹ : 3335, 2940, 1628, 1619, 1560,1426, 1366, 1299, 992.

EXAMPLE 66N-[5-(4-Piperidinomethyl-2-pyridyloxy)pentyl]pyrazole-4-carboxamide

Following a procedure similar to that described in Example 64, but using5-(4-piperidinomethyl-2-pyridyloxy)pentylamine and 4-pyrazolecarboxylicacid as starting materials, in relative proportions similar to thoseused in that Example, the title compound was obtained as a white powder,melting at 105°-106° C., in a yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.42-1.60 (4H,multiplet); 1.60-1.74 (6H, multiplet); 1.76-1.88 (2H, multiplet);2.40-2.63 (4H, multiplet); 3.43 (2H, quartet, J=6.7 Hz); 3.51 (2H,singlet); 4.27 (2H, triplet, J=6.3 Hz); 6.15-6.25 (1H, broad); 6.75 (1H,singlet); 6.88 (1H, doublet, J=5.3 Hz); 7.96 (2H, singlet); 8.07 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3460, 2930, 1640, 1610, 1570, 1418, 1320.

EXAMPLE 67N-[3-(4-Piperidinomethyl-2-pyridyloxy)propyl]-2-(2-acetoxyethylthio)acetamide67(a) N-[3-(4-Piperidinomethyl-2-pyridyloxy)propyl]-2-chloroacetamide

1.68 ml of triethylamine were added to a solution of 3.00 g of3-(4-piperidinomethyl-2-pyridyloxy)propylamine in 60 ml of ethylacetate, and the resulting mixture was cooled with ice, after which 0.96ml of 2-chloroacetyl chloride was added. The reaction mixture was thenstirred at room temperature for 1 hour, after which it was mixed withwater and the aqueous mixture was extracted with ethyl acetate. Theextract was concentrated by evaporation under reduced pressure, and theconcentrate was purified by column chromatography through silica gel,using a 1:9 by volume mixture of methanol and ethyl acetate as theeluent, to give 3.40 g (yield 87%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.52 (2H,multiplet); 1.52-1.66 (4H, multiplet); 2.94-3.07 (2H, multiplet);2.33-2.44 (4H, multiplet); 3.43 (2H, singlet); 3.48 (2H, triplet ofdoublets, J=6.6 & 5.9 Hz); 4.07 (2H, singlet); 4.44 (2H, triplet, J=5.9Hz); 6.76 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 7.36-7.58 (1H,broad); 8.06 (1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum(CHCl₃), ν_(max) cm⁻¹ : 3425, 2925, 1730, 1660, 1610, 1530, 1420.

67(b)N-[3-(4-Piperidinomethyl-2-pyridyloxy)propyl]-2-(2-hydroxyethylthio)acetamide

0.12 ml of 2-mercaptoethanol was added to a solution of 0.13 g of 85%potassium hydroxide and 0.50 g ofN-[3-(4-piperidinomethyl-2-pyridyloxy)propyl]-2-chloroacetamide[prepared as described in step (a) above] in 10 ml methanol, and theresulting mixture was stirred at room temperature for 1 hour. At the endof this time, the reaction mixture was concentrated by evaporation underreduced pressure, the concentrate was mixed with water, and theresulting aqueous mixture was extracted with chloroform. The extract wasconcentrated by evaporation under reduced pressure, and the residue waspurified by column chromatography through silica gel, using a 1:9 byvolume mixture of ethanol and chloroform as the eluent, to give 0.43 g(yield 77%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.52 (2H,multiplet); 1.52-1.66 (4H, multiplet); 1.95-2.09 (2H, multiplet);2.31-2.85 (4H, multiplet); 2.79 (2H, triplet, J=5.6 Hz); 3.30 (2H,singlet); 3.42 (2H, singlet); 3.49 (2H, triplet of doublets, J=6.6 & 5.9Hz); 3.82 (2H, triplet, J=5.6 Hz); 4.42 (2H, triplet, J=5.9 Hz); 6.77(1H, singlet); 6.88 (1H, doublet, J=5.3 Hz); 7.48-7.66 (1H, broad); 8.06(1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃) ν_(max)cm⁻¹ : 3350, 2925, 1650, 1610, 1560, 1520, 1420.

67(c)N-[3-(4-Piperidinomethyl-2-pyridyloxy)propyl]-2-(2-acetoxyethylthio)acetamide

0.49 g ofN-[3-(4-piperidinomethyl-2-pyridyloxy)propyl]-2-(2-hydroxyethylthio)acetamide[prepared as described in step (b) above] was added to a mixture of 0.48ml of acetic anhydride and 0.43 ml of pyridine, and the resultingmixture was warmed at 60° C. for 2 hours. At the end of this time, thereaction mixture was poured into ice-water and a saturated aqueoussolution of sodium hydrogencarbonate was added to it. The resultingaqueous mixture was extracted with ethyl acetate. The extract wasconcentrated by evaporation under reduced pressure, and the concentratewas purified by column chromatography through silica gel, using a 1:9 byvolume mixture of methanol and ethyl acetate as the eluent, to give 0.41g (yield 75%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.51 (2H,multiplet); 1.51-1.67 (4H, multiplet); 1.93-2.09 (2H, multiplet); 2.05(3H, singlet); 2.31-2.43 (4H, multiplet); 2.80 (2H, triplet, J=5.9 Hz);3.30 (2H, singlet); 3.42 (2H, singlet); 3.46 (2H, triplet of doublets,J=6.6 & 5.9 Hz); 4.24 (2H, triplet, J=6.6 Hz); 4.42 (2H, triplet, J=5.9Hz); 6.77 (1H, singlet); 6.88 (1H, doublet, J=5.3 Hz); 7.38-7.54 (1H,broad); 8.06 (1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum(CHCl₃), ν_(max) cm⁻¹ : 3375, 2925, 1740, 1660, 1610, 1520, 1420, 1220.

The title compound, prepared as described above, was dissolved in ethylacetate, and a 4N ethyl acetate solution of hydrogen chloride was addedto the solution. The crystals which precipitated were collected byfiltration, to give the hydrochloride of the title compound, melting at121°-128° C.

EXAMPLE 68N-[3-(4-Piperidinomethyl-2-pyridyloxy)propyl]-2-(2-hydroxyethylthio)acetamide

A mixture of 0.38 g of 3-(4-piperidinomethyl-2-pyridyloxy)propylamineand 0.18 g of 1,4-oxathian-2-one was added to 10 ml of ethanol, and theresulting mixture was heated under reflux for 2 hours. At the end ofthis time, the reaction mixture was concentrated by evaporation underreduced pressure. The concentrate was mixed with water, and theresulting aqueous mixture was extracted with ethyl acetate. The extractwas concentrated by evaporation under reduced pressure, and theconcentrate was purified by column chromatography through silica gel,using a 1:9 by volume mixture of methanol and methylene chloride as theeluent, to give 0.49 g (yield 88%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.52 (2H,multiplet); 1.52-1.66 (4H, multiplet); 1.95-2.09 (2H, multiplet);2.31-2.85 (4H, multiplet); 2.79 (2H, triplet, J=5.6 Hz); 3.30 (2H,singlet); 3.42 (2H, singlet); 3.49 (2H, triplet of doublets, J=6.6 & 5.9Hz); 3.82 (2H, triplet, J=5.6 Hz); 4.42 (2H, triplet, J=5.9 Hz); 6.77(1H, singlet); 6.88 (1H, doublet, J=5.3 Hz); 7.48-7.66 (1H, broad); 8.06(1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max)cm⁻¹ : 3350, 2925, 1650, 1610, 1560, 1520, 1420.

EXAMPLE 69N-[4-(4-Piperidinomethyl-2-pyridyloxy)butyl]-2-(2-acetoxyethylthio)acetamide69(a) N-[4-(4-Piperidinomethyl-2-pyridyloxy)butyl]-2-chloroacetamide

Following a procedure similar to that described in Example 67(a), butusing 4-(4-piperidinomethyl-2-pyridyloxy)butylamine and 2-chloroacetylchloride as starting materials, in relative proportions similar to thoseused in that Example, the title compound was obtained as a white powder,melting at 59°-63° C., in an 80% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.51 (2H,multiplet); 1.51-1.66 (4H, multiplet); 1.66-1.91 (4H, multiplet);2.31-2.44 (4H, multiplet); 3.35-3.47 (2H, multiplet); 3.41 (2H,singlet); 4.05 (2H, singlet); 4.31 (2H, triplet, J=5.9 Hz); 6.63-6.81(1H, broad); 6.71 (1H, singlet); 6.87 (1H, triplet, J=5.3 Hz); 8.05 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ :3325, 2925, 1670, 1610, 1530, 1420.

69(b)N-[4-(4-Piperidinomethyl-2-pyridyloxy)butyl]-2-(2-hydroxyethylthio)acetamide

Following a procedure similar to that described in Example 67(b), butusing 4-(4-piperidinomethyl-2-pyridyloxy)butyl-2-chloroacetamide[prepared as described in step (a) above] and 2-mercaptoethanol asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as an oil in aquantitative yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.50 (2H,multiplet); 1.59-1.64 (4H, multiplet); 1.64-1.91 (5H, multiplet);2.31-2.44 (4H, multiplet); 2.77 (2H, triplet, J=5.9 Hz); 3.27 (2H,singlet); 3.31-3.45 (2H, multiplet); 3.41 (2H, singlet); 3.81 (2H,triplet, J=5.9 Hz); 4.30 (2H, triplet, J=5.9 Hz); 6.74 (1H, singlet);6.86 (1H, doublet, J=5.3 Hz); 6.86-7.14 (1H, broad); 8.04 (1H, doublet,J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3350,2925, 1660, 1610, 1540, 1520, 1420, 1300.

69(c)N-[4-(4-Piperidinomethyl-2-pyridyloxy)butyl]-2-(2-acetoxyethylthio)acetamide

Following a procedure similar to that described in Example 67(c), butusingN-[4-(4-piperidinomethyl-2-pyridyloxy)butyl]-2-(2-hydroxyethylthio)acetamide[prepared as described in step (b) above] and acetic anhydride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as an oil in an 84% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.51 (2H,multiplet); 1.51-1.64 (4H, multiplet); 1.64-1.89 (4H, multiplet); 2.07(3H, singlet); 2.31-2.44 (4H, multiplet); 2.79 (2H, triplet, J=6.6 Hz);3.27 (2H, singlet); 3.32-3.43 (2H, multiplet); 3.41 (2H, singlet); 4.24(2H, triplet, J=6.6 Hz); 4.31 (2H, triplet, J=5.9 Hz); 6.70 (1H,singlet); 6.81-6.94 (1H, broad); 6.87 (2H, doublet, J=5.3 Hz); 8.05 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3375, 2925, 1740, 1660, 1610, 1560, 1520, 1420.

The title compound, prepared as described above, was dissolved in ethylacetate, and a 4N ethyl acetate solution of hydrogen chloride was addedto the solution. The crystals which precipitated were collected byfiltration, to give the hydrochloride of the title compound, melting at91°-98° C.

EXAMPLE 70N-[5-(4-Piperidinomethyl-2-pyridyloxy)pentyl]-2-(2-acetoxyethylthio)acetamide70(a)N-[5-(4-Piperidinomethyl-2-pyridyloxy)pentyl]-2-(2-hydroxyethylthio)acetamide

Following a procedure similar to that described in Example 68, but using5-(4-piperidinomethyl-2-pyridyloxy)pentylamine and 1,4-oxathian-2-one asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as an oil in a 78% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-2.00 (13H,multiplet); 2.31-2.43 (4H, multiplet); 2.77 (2H, triplet, J=5.9 Hz);3.26 (2H, singlet); 3.33 (2H, triplet of doublets, J=6.6 & 5.9 Hz); 3.40(2H, singlet); 3.81 (2H, triplet, J=5.9 Hz); 4.26 (2H, triplet, J=5.9Hz); 6.74 (1H, singlet); 6.78-6.95 (1H, broad); 6.84 (1H, triplet, J=5.3Hz); 8.04 (1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃),ν_(max) cm⁻¹ : 3375, 2925, 1660, 1610, 1560, 1520, 1420.

70(b)N-[5-(4-Piperidinomethyl-2-pyridyloxy)pentyl]-2-(2-acetoxyethylthio)acetamide

Following a procedure similar to that described in Example 67(c), butusingN-[5-(4-piperidinomethyl-2-pyridyloxy)pentyl]-2-(2-hydroxyethylthio)acetamide[prepared as described in step (a) above] and acetic anhydride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as an oil in a 90% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.64 (10H,multiplet); 1.72-1.86 (2H, multiplet); 2.07 (3H, singlet); 2.31-2.41(4H, multiplet); 2.79 (2H, triplet, J=6.6 Hz); 3.27 (2H, singlet); 3.32(2H, quartet, J=6.6 Hz); 4.19-4.31 (4H, multiplet); 6.69 (1H, singlet);6.69-6.88 (1H, broad); 6.85 (1H, doublet, J=5.3 Hz); 8.05 (1H, doublet,J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3375,2925, 1740, 1660, 1610, 1520, 1420.

EXAMPLE 71N-[4-(4-Piperidinomethyl-2-pyridyloxy)butyl]-2-(2-propionyloxyethylthio)acetamide

Following a procedure similar to that described in Example 67(c), butusingN-[4-(4-piperidinomethyl-2-pyridyloxy)butyl]-2-(2-hydroxyethylthio)acetamide[prepared as described in Example 69(b)] and propionic anhydride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as an oil in an 80% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.14 (3H, triplet,J=7.3 Hz); 1.35-1.88 (10H, multiplet); 2.26-2.42 (4H, multiplet); 2.35(2H, quartet, J=7.3 Hz); 2.79 (2H, triplet, J=6.3 Hz); 3.27 (2H,singlet); 3.32-3.43 (2H, multiplet); 3.41 (2H, singlet); 4.25 (2H,triplet, J=6.3 Hz); 4.30 (2H, triplet, J=6.6 Hz); 6.70 (1H, singlet);6.75-6.98 (1H, broad); 6.86 (1H, doublet, J=5.3 Hz); 8.04 (1H, doublet,J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3375,2925, 1730, 1660, 1610, 1560, 1520, 1420.

EXAMPLE 72N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-5-(2-acetoxyethylthio)pentanamide72(a)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-5-chloropentanamide

Following a procedure similar to that described in Example 67(a), butusing 4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine and5-chlorovaleryl chloride as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 93% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.50 (2H,multiplet); 1.50-1.63 (4H, multiplet); 1.74-1.86 (4H, multiplet);2.18-2.28 (2H, multiplet); 2.28-2.42 (4H, multiplet); 3.41 (2H,singlet); 3.50-3.59 (2H, multiplet); 4.04 (2H, triplet, J=5.9 Hz); 4.93(2H, doublet, J=6.6 Hz); 5.62-5.74 (1H, multiplet); 5.77-5.90 (1H,multiplet); 5.92-6.20 (1H, broad); 6.73 (1H, singlet); 6.89 (1H,doublet, J=5.3 Hz); 8.03 (1H, doublet, J=5.3 Hz). Infrared AbsorptionSpectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 2950, 1660, 1610, 1560, 1510,1400.

72(b)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-5-(methoxycarbonylmethylthio)pentanamide

344 mg of sodium hydride (as a 55% w/w dispersion in mineral oil) wereadded, whilst ice-cooling and in an atmosphere of nitrogen, to asolution of 0.35 ml of methyl thioglycolate in 90 ml of tetrahydrofuran,and the resulting mixute was stirred at room temperature for 30 minutes.At the end of this time, it was cooled with ice, and a solution of 2.94g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-5-chloropentanamide[prepared as described in step (a) above] in 30 ml of tetrahydrofuranwas added dropwise to the mixture. The reaction mixture was then stirredat room temperature for 2 hours, after which the solvent was removed bydistillation under reduced pressure. The residue was mixed with water,and the resulting aqueous mixture was extracted with ethyl acetate. Theextract was concentrated by evaporation under reduced pressure, and theresidue was purified by column chromatography through silica gel, usinga 1:19 by volume mixture of methanol and ethyl acetate as the eluent, togive 2.84 g (yield 89%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.48 (2H,multiplet); 1.48-1.87 (8H, multiplet); 2.23 (2H, triplet, J=7.3 Hz);2.32-2.46 (4H, multiplet); 2.66 (2H, triplet, J=7.3 Hz); 3.23 (2H,singlet); 3.42 (2H, singlet); 3.75 (3H, singlet); 4.05 (2H, triplet,J=5.9 Hz); 4.94 (2H, doublet, J=6.6 Hz); 5.63-5.76 (1H, multiplet);5.79-5.92 (1H, multiplet); 5.95-6.18 (1H, broad); 6.75 (1H, singlet);6.91 (1H, doublet, J=5.3 Hz); 8.05 (1H, doublet, J=5.3 Hz). InfraredAbsorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 2925, 1730, 1660,1610, 1560, 1510, 1400.

72(c)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2butenyl]-5-(2-hydroxyethylthio)pentanamide

0.21 g of sodium borohydride was added to a solution of 1.98 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-5-(methoxycarbonylmethylthio)pentanamide[prepared as described in step (b) above] in 40 ml of tetrahydrofuran,and 8 ml of methanol were added dropwise to the mixture, whilstice-cooling; it was then stirred at room temperature for 3 hours. At theend of this time, the reaction mixture was concentrated by evaporationunder reduced pressure, and the residue was mixed with water. Theresulting aqueous mixture was extracted with ethyl acetate, and theextract was freed from the solvent by distillation under reducedpressure. The residue was purified by column chromatography throughsilica gel, using a 1:9 by volume mixture of methanol and methylenechloride as the eluent, to give 1.51 g (yield 63%) of the title compoundas an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-2.09 (11H,multiplet); 2.22 (2H, triplet, J=7.3 Hz); 2.26-2.47 (4H, multiplet);2.54 (2H, triplet, J=7.3 Hz); 2.72 (2H, triplet, J=5.9 Hz); 3.41 (2H,singlet); 3.72 (2H, triplet, J=5.9 Hz); 4.04 (2H, triplet, J=5.9 Hz);4.93 (2H, doublet, J=6.6 Hz); 5.62-5.75 (1H, multiplet); 5.78-5.90 (1H,multiplet); 5.97-6.19 (1H, broad); 6.74 (1H, singlet); 6.90 (1H,doublet, J=5.3 Hz); 8.04 (1H, doublet, J=5.3 Hz). Infrared AbsorptionSpectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 2925, 1660, 1610, 1560, 1510,1420.

72(d)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-5-(2-acetoxyethylthio)pentanamide

Following a procedure similar to that described in Example 67(c), butusingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-5-(2-hydroxyethylthio)pentanamide[prepared as described in step (c) above] and acetic anhydride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained as an oil in a 92% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.86 (10H,multiplet); 2.07 (3H, singlet); 2.21 (2H, triplet, J=7.3 Hz); 2.30-2.47(4H, multiplet); 2.57 (2H, triplet, J=7.3 Hz); 2.73 (2H, doublet ofdoublets, J=7.3 & 6.6 Hz); 3.41 (2H, singlet); 4.03 (2H, triplet, J=5.8Hz); 4.20 (2H, doublet of doublets, J=7.3 & 6.6 Hz); 4.93 (2H, doublet,J=6.6 Hz); 5.58-5.76 (1H, multiplet); 5.78-5.90 (1H, multiplet);5.95-6.16 (1H, broad); 6.73 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz);8.04 (1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃),ν_(max) cm⁻¹ : 3375, 2950, 1660, 1610, 1560, 1520, 1420.

EXAMPLE 73N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-6-(2-acetoxyethylthio)hexanamide73(a)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-6-bromohexanamide

Following a procedure similar to that described in Example 67(a), butusing N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine] and6-bromohexanoyl bromide as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in an 86% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.77 (10H,multiplet); 1.82-1.95 (2H, multiplet); 2.20 (2H, triplet, J=7.3 Hz);2.28-2.43 (4H, multiplet); 3.41 (2H, triplet, J=5.3 Hz); 4.04 (2H,triplet, J=5.9 Hz); 4.93 (2H, doublet, J=6.6 Hz); 5.62-5.76 (1H,multiplet); 5.78-5.90 (1H, multiplet); 5.92-6.11 (1H, broad); 6.73 (1H,singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.03 (1H, doublet, J=5.3 Hz).Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3350, 2925, 1660,1610, 1560, 1510, 1420, 1300.

73(b)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-6-(2-hydroxyethylthio)hexanamide

Following a procedure similar to that described in Example 67(b), butusingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-6-bromohexanamide[prepared as described in step (a) above] and 2-mercaptoethanol asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in a 94% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.74 (12H,multiplet); 1.63-2.19 (1H, broad); 2.19 (2H, triplet, J=7.3 Hz);2.29-2.45 (4H, multiplet); 2.53 (2H, triplet, J=7.3 Hz); 2.71 (2H,triplet, J=5.9 Hz); 3.41 (2H, singlet); 3.72 (2H, triplet, J=5.9 Hz);4.03 (2H, doublet of doublets, J=6.6 & 5.9 Hz); 4.92 (2H, doublet, J=6.6Hz); 5.61-5.74 (1H, multiplet); 5.77-5.89 (1H, multiplet); 5.93-6.13(1H, broad); 6.73 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.03 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3450, 2925, 1660, 1610, 1560, 1510, 1420.

73(c)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-6-(2-acetoxyethylthio)hexanamide

Following a procedure similar to that described in Example 67(c), butusingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-6-(2-hydroxyethylthio)hexanamide[prepared as described in step (b) above] and acetic anhydride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in an 87% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.74 (12H,multiplet); 2.07 (3H, singlet); 2.19 (2H, triplet, J=7.3 Hz); 2.31-2.44(4H, multiplet); 2.56 (2H, triplet, J=7.3 Hz); 2.72 (2H, triplet, J=7.3Hz); 3.41 (2H, singlet); 4.03 (2H, doublet of doublets, J=6.6 & 5.9 Hz);4.20 (2H, triplet, J=7.3 Hz); 4.92 (2H, doublet, J=6.6 Hz); 5.62-5.74(1H, multiplet); 5.78-5.90 (1H, multiplet); 5.92-6.12 (1H, broad); 6.73(1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.03 (1H, doublet, J=5.3Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3450, 2925,1740, 1660, 1610, 1560, 1510, 1420.

EXAMPLE 74N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(3-acetoxyethylthio)acetamide74 (a)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-chloroacetamide

0.54 ml of triethylamine was added to a solution of 1.00 g of4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine in 20 ml of ethylacetate, and the resulting mixture was cooled. 0.31 ml of 2-chloroacetylchloride were then added to the mixture. The reaction mixture was thenstirred at room temperature for 1 hour, after which it was mixed withwater, and the aqueous mixture was extracted with ethyl acetate. Theextract was concentrated by evaporation under reduced pressure, and theresidue was purified by column chromatography through silica gel, usinga 1:19 by volume mixture of methanol and ethyl acetate as the eluent, togive 0.94 g (yield 73%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.50-1.64 (4H, multiplet); 2.30-2.43 (2H, multiplet);2.30-2.43 (4H, multiplet); 3.41 (2H, singlet); 4.06 (2H, singlet); 4.11(2H, triplet, J=6.6 Hz); 4.94 (2H, doublet, J=6.6 Hz); 5.62-5.75 (1H,multiplet); 5.84-5.97 (1H, multiplet); 6.69-6.92 (1H, broad); 6.74 (1H,singlet); 6.88 (1H, doublet, J=4.6 Hz); 8.06 (1H, doublet, J=4.6 Hz).Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3420, 2920, 1665,1610, 1525, 1400, 1285.

74(b)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(acetylthio)acetamide

A solution of 0.47 ml of thioacetic acid in 20 ml of tetrahydrofuran wasadded dropwise, whilst ice-cooling and in an atmosphere of nitrogen, toa suspension of 0.29 g of sodium hydride (as a 55% w/w dispersion inmineral oil) in 20 ml of tetrahydrofuran, and the resulting mixture wasstirred at room temperature for 30 minutes. At the end of this time, asolution of 2.00 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-chloroacetamide[prepared as described in step (a) above] in 20 ml of tetrahydrofuranwas added dropwise to the mixture, whilst ice-cooling, after which itwas stirred at room temperature for 30 minutes. The reaction mixture wasthen concentrated by evaporation under reduced pressure, the residue wasmixed with water, and the resulting aqueous mixture was extracted withethyl acetate. The extract was concentrated by evaporation under reducedpressure, and the concentrate was purified by column chromatographythrough silica gel, using a 1:19 by volume mixture of methanol and ethylacetate as the eluent, to give 1.72 g (yield 77%) of the title compoundas an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.50 (2H,multiplet); 1.50-1.67 (4H, multiplet); 2.32-2.43 (4H, multiplet); 2.41(3H, singlet); 3.42 (2H, singlet); 3.57 (2H, singlet); 4.04 (2H,triplet, J=5.9 Hz); 4.93 (2H, triplet, J=6.6 Hz); 5.57-5.71 (1H,multiplet); 5.81-5.91 (1H, multiplet); 6.35-6.66 (1H, broad); 6.75 (1H,singlet); 6.90 (1H, doublet, J=5.3 Hz); 8.08 (1H, doublet, J=5.3 Hz).Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3400, 2925, 1680,1610, 1560, 1520, 1400.

74(c) N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(3-hydroxypropylthio)acetamide

5 ml of a methanolic solution containing 0.26 g of a 28% w/v sodiummethoxide solution were added, whilst ice-cooling, to a solution of 0.50g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(acetylthio)acetamide[prepared as described in step (b) above] in 5 ml of methanol, and theresulting solution was stirred for 20 minutes. At the end of this time,a solution of 0.11 ml of 3-chloro-1-propanol in 5 ml of methanol, wasadded, and the reaction mixture was heated under reflux for 5 hours. Thesolvent was then removed by distillation under reduced pressure. Theresidue thus obtained was mixed with water, and the aqueous mixture wasextracted with ethyl acetate. The extract was concentrated byevaporation under reduced pressure, and the residue was purified bycolumn chromatography through silica gel, using a 1:9 by volume mixtureof methanol and methylene chloride as the eluent, to give 0.42 g (yield81%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.51 (2H,multiplet); 1.51-1.66 (4H, multiplet); 1.54-2.02 (4H, broad); 1.84 (2H,triplet of doublets, J=7.3 & 5.9 Hz); 2.32-2.45 (4H, multiplet); 2.68(2H, triplet, J=7.3 Hz); 3.24 (2H, singlet); 3.41 (2H, singlet); 3.73(2H, triplet, J=5.9 Hz); 4.07 (2H, doublet of doublets, J=6.6 & 5.9 Hz);4.93 (2H, doublet, J=6.6 Hz); 5.61-5.78 (1H, multiplet); 5.82-5.94 (1H,multiplet); 6.76 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 7.70-7.25(1H, broad); 8.06 (1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum(CHCl₃), ν_(max) cm⁻¹ : 3375, 2950, 1660, 1610, 1560, 1520, 1420.

74(d)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(3-acetoxypropylthio)acetamide

Following a procedure similar to that described in Example 67(c), butusingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(3-hydroxypropylthio)acetamide[prepared as described in step (c) above] and acetic anhydride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in an 87% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.38-1.51 (2H,multiplet); 1.51-1.66 (4H, multiplet); 1.91 (2H, triplet of doublets,J=7.3 & 5.9 Hz); 2.05 (3H, singlet); 2.31-2.43 (4H, multiplet); 2.61(2H, triplet, J=7.3 Hz); 3.23 (2H, singlet); 3.41 (2H, singlet);4.03-4.20 (4H, multiplet); 4.94 (2H, doublet, J=6.6 Hz); 5.60-5.77 (1H,multiplet); 5.81-5.94 (1H, multiplet); 6.74 (1H, singlet); 6.89 (1H,doublet, J=5.3 Hz); 6.92-7.10 (1H, broad); 8.06 (1H, doublet, J=5.3 Hz).Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3375, 2950, 1715,1660, 1610, 1560, 1520, 1420.

The title compound, prepared as described above, was dissolved in ethylacetate, and a 4N ethyl acetate solution of hydrogen chloride was addedto the resulting solution. The crystals which precipitated werecollected by filtration, to give the hydrochloride of the titlecompound, melting at 110°-124° C.

EXAMPLE 75N-[4-(4-Dimethylaminomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide75(a)N-[4-(4-Dimethylaminomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide

Following a procedure similar to that described in Example 68, but using4-(4-dimethylaminomethyl-2-pyridyloxy)-cis-2-butenylamine and1,4-oxathian-2-one as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedin a 53% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.61-2.27 (1H, broadsinglet); 2.26 (6H, singlet); 2.77 (2H, triplet, J=5.9 Hz); 3.29 (2H,singlet); 3.40 (2H, singlet); 4.07 (2H, doublet of doublets, J=6.6 & 5.9Hz); 4.95 (2H, doublet, J=6.6 Hz); 5.61-5.73 (1H, multiplet); 5.76-5.87(1H, multiplet); 6.76 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz);7.07-7.26 (1H, broad); 8.08 (1H, doublet, J=5.3 Hz). Infrared AbsorptionSpectrum (CHCl₃), ν_(max) cm⁻¹ : 3400, 2975, 1660, 1610, 1560, 1520,1420.

75(b)N-[4-(4-Dimethylaminomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide

Following a procedure similar to that described in Example 67(c), butusingN-[4-(4-dimethylaminomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide[prepared as described in step (a) above] and acetic anhydride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in a 58% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 2.09 (3H, singlet);2.26 (6H, singlet); 2.81 (2H, triplet, J=6.6 Hz); 3.30 (2H, singlet);3.40 (2H, singlet); 4.10 (2H, doublet of doublets, J=6.6 & 5.9 Hz); 4.26(2H, triplet, J=6.6 Hz); 4.96 (2H, doublet, J=6.6 Hz); 5.62-5.75 (1H,multiplet); 5.82-5.96 (1H, multiplet); 6.73 (1H, singlet); 6.89 (1H,doublet, J=5.3 Hz); 6.90-7.13 (1H, broad); 8.10 (1H, doublet, J=5.3 Hz).Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3375, 2950, 2800,1740, 1660, 1610, 1560, 1510, 1400.

EXAMPLE 76N-{4-[4-(1-Pyrrolidinylmethyl)-2-pyridyloxy]-cis-2-butenyl}-2-(2-acetoxyethylthio)acetamide

Following a procedure similar to that described in Example 68, but using4-[4-(1-pyrrolidinylmethyl)-2-pyridyloxy]-cis-2-butenylamine and1,4-oxathian-2-one as starting materials, in relative proportionssimilar to those used in that Example,N-{4-[4-(1-pyrrolidinylmethyl)-2-pyridyloxy]-cis-2-butenyl}-2-(2-hydroxyethylthio)acetamidewas obtained. This product was reacted with acetic anhydride in the samemanner and same relative proportions as described in Example 67(c), togive the title compound in a 42% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.71-1.84 (4H,multiplet); 2.07 (3H, singlet); 2.46-2.57 (4H, multiplet); 2.79 (2H,triplet, J=6.3 Hz); 3.28 (2H, singlet); 3.58 (2H, singlet); 4.08 (2H,triplet, J=6.6 Hz); 4.24 (2H, triplet, J=6.3 Hz); 4.94 (2H, doublet,J=6.6 Hz); 5.61-5.73 (1H, multiplet); 5.81-5.94 (1H, multiplet); 6.74(1H, singlet); 6.90 (1H, doublet, J=5.3 Hz); 6.90-7.09 (1H, broad); 8.07(1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max)cm⁻¹ : 3400, 2950, 2800, 1740, 1660, 1610, 1560, 1520, 1420.

EXAMPLE 77N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylsulfinyl)acetamide

77 μl of methanesulfonic acid was added to a solution of 0.50 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide(prepared as described in Example 2) in 5.5 ml of 1,2-dichloroethane,and the resulting mixture was cooled to -10° C. 0.28 g of3-chloroperoxybenzoic acid (purity: 80%) was then added, and thereaction mixture was stirred, whilst keeping the temperature in therange from -10° C. to -5° C., for 2 hours. At the end of this time, itwas washed with a 10% w/v aqueous solution of sodium hydrogensulfite,with a saturated aqueous solution of sodium hydrogencarbonate and with asaturated aqueous solution of sodium chloride, in that order. Thesolvent was then removed by distillation under reduced pressure, and theresulting residue was purified by column chromatography through silicagel, using a 1:9 by volume mixture of ethanol and chloroform as theeluent, to give 0.38 g (yield 73%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.49 (2H,multiplet); 1.49-1.64 (4H, multiplet); 2.09 (3H, singlet); 2.31-2.42(4H, multiplet); 3.12-3.18 (2H, multiplet); 3.39 (1H, doublet, J=13.2Hz); 3.41 (2H, singlet); 3.73 (1H, doublet, J=13.2 Hz); 4.10 (2H,triplet, J=5.9 Hz); 4.38-4.60 (2H, multiplet); 4.93 (2H, doublet, J=5.3Hz); 5.61-5.73 (1H, multiplet); 5.79-5.90 (1H, multiplet); 6.73 (1H,singlet); 6.88 (1H, doublet, J=5.3 Hz); 7.05-7.24 (1H, broad); 8.06 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3400, 2950, 1740, 1670, 1610, 1560, 1410, 1310, 1220.

EXAMPLE 78N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylsulfonyl)acetamide

72 μl of methanesulfonic acid were added to a solution of 0.47 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide(prepared as described in Example 2) in 5.5 ml of 1,2-dichloroethane.The resulting mixture was cooled to -10° C. 0.51 g of3-chloroperoxybenzoic acid (purity: was added to the reaction mixture,which was then stirred at a temperature in the range from -10° C. to -5°C. for 2 hours. At the end of this time, the reaction mixture was washedwith a 10% w/v aqueous solution of sodium hydrogensulfite, with asaturated aqueous solution of sodium hydrogencarbonate and with asaturated aqueous solution of sodium chloride, in that order, and thenthe solvent was removed by distillation under reduced pressure. Theresidue was purified by column chromatography through silica gel, usinga 1:9 by volume mixture of ethanol and chloroform as the eluent, to give0.40 g (yield 40%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.50-1.70 (4H, multiplet); 2.11 (3H, singlet); 2.30-2.41(4H, multiplet); 3.41 (2H, singlet); 3.55 (2H, triplet, J=5.6 Hz); 3.93(2H, singlet); 4.09 (2H, triplet, J=5,6 Hz); 4.93 (2H, doublet, J=5.9Hz); 5.61-5.73 (1H, multiplet); 5.80-5.93 (1H, multiplet); 6.75 (1H,singlet); 6.90 (1H, doublet, J=5.3 Hz); 7.32-7.43 (1H, broad); 8.06 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃) ν_(max) cm⁻¹ :3300, 2950, 1740, 1680, 1610, 1560, 1400, 1320.

EXAMPLE 79N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(3,3-dimethylbutyryloxy)ethylthio)acetamide

Following a procedure similar to that described in Example 7, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide(prepared as described in Example 1) and 3,3-dimethylbutyryl chloride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in an 83% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.02 (9H, singlet);1.37-1.50 (2H, multiplet); 1.50-1.65 (4H, multiplet); 2.21 (2H,singlet); 2.31-2.43 (4H, multiplet); 2.79 (2H, triplet, J=6.6 Hz); 3.28(2H, singlet); 3.41 (2H, singlet); 4.08 (2H, triplet, J=5.9 Hz); 4.23(2H, triplet, J=6.6 Hz); 4.94 (2H, doublet, J=5.9 Hz); 5.60-5.72 (1H,multiplet); 5.81-5.93 (1H, multiplet); 6.73 (1H, singlet); 6.88 (1H,doublet, J=5.3 Hz); 6.92-7.10 (1H, broad); 8.06 (1H, doublet, J=5.3 Hz).Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3375, 2925, 1730,1660, 1610, 1560, 1520, 1400.

The title compound, prepared as described above, was dissolved in ethylacetate and treated with an equivalent amount of a 4N solution ofhydrogen chloride in ethyl acetate to give the hydrochloride of thetitle compound, melting at 106°-109° C.

EXAMPLE 80N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(2-methylpropionyloxy)ethylthio]acetamide

Following a procedure similar to that described in Example 7, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide(prepared as described in Example 1) and 2-methylpropionyl chloride asstarting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in a 73% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.17 (6H, doublet,J=7.3 Hz); 1.37-1.52 (2H, multiplet); 1.50-1.66 (4H, multiplet);2.31-2.44 (4H, multiplet); 2.56 (1H, septet, J=7.3 Hz); 2.79 (2H,triplet, J=6.6 Hz); 3.28 (2H, singlet); 3.42 (2H, singlet); 4.08 (2H,triplet, J=6.3 Hz); 4.24 (2H, triplet, J=6.6 Hz); 4.94 (2H, doublet,J=6.6 Hz); 5.60-5.74 (1H, multiplet); 5.81-5.93 (1H, multiplet); 6.73(1H, singlet); 6.88 (1H, doublet, J=5.3 Hz); 6.93-7.07 (1H, broad); 8.06(1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max)cm⁻¹ : 3375, 2925, 1730, 1660, 1610, 1560, 1520, 1400.

The title compound, prepared as described above, was dissolved in ethylacetate and treated with an equimolar amount of a 4N solution ofhydrogen chloride in ethyl acetate to give the hydrochloride of thetitle compound, melting at 93°-96° C.

EXAMPLE 81N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(2,2-dimethylpropionyloxy)ethylthio]acetamide

Following a procedure similar to that described in Example 7, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide(prepared as described in Example 1) and 2,2-dimethylpropionyl chlorideas starting materials, in relative proportions similar to those used inthat Example, the title compound was obtained in a 63% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.20 (9H, singlet);1.38-1.52 (2H, multiplet); 1.52-1.69 (4H, multiplet); 2.28-2.53 (4H,multiplet); 2.79 (2H, triplet, J=6.6 Hz); 3.28 (2H, singlet); 3.45 (2H,singlet); 4.09 (2H, triplet, J=6.6 Hz); 4.22 (2H, triplet, J=6.6 Hz);4.94 (2H, doublet, J=6.6 Hz); 5.64-5.73 (1H, multiplet); 5.82-5.93 (1H,multiplet); 6.75 (1H, singlet); 6.91 (1H, doublet, J=5.1 Hz); 6.93-7.09(1H, broad); 8.07 (1H, doublet, J=5.1 Hz). Infrared Absorption Spectrum(CHCl₃), ν_(max) cm⁻¹ : 3375, 2925, 1720, 1660, 1610, 1540, 1520, 1480,1400.

The title compound, prepared as described above, was dissolved in ethylacetate and treated with an equimolar amount of a 4N solution ofhydrogen chloride in ethyl acetate to give the hydrochloride of thetitle compound, melting at 93°-97° C.

EXAMPLE 82N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-butyryloxyethylthio)acetamide

Following a procedure similar to that described in Example 7, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide(prepared as described in Example 1) and butyryl chloride as startingmaterials, in relative proportions similar to those used in thatExample, the title compound was obtained in an 88% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 0.94 (3H, triplet,J=7.3 Hz); 1.34-1.78 (8H, multiplet); 2.29-2.39 (4H, multiplet); 2.30(2H, triplet, J=7.3 Hz); 2.79 (2H, triplet, J=6.6 Hz); 3.28 (2H,singlet); 3.41 (2H, singlet); 4.08 (2H, doublet of doublets, J=7.3 & 6.6Hz); 4.24 (2H, triplet, J=6.6 Hz); 4.93 (2H, doublet, J=7.9 Hz);5.60-5.78 (1H, multiplet); 5.81-5.94 (1H, multiplet); 6.73 (1H,singlet); 6.89 (1H, doublet, J=5.3 Hz); 6.92-7.10 (1H, broad); 8.07 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3400, 2950, 1740, 1660, 1610, 1560, 1520, 1420.

EXAMPLE 83N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylsulfinyl)acetamide

Following a procedure similar to that described in Example 77, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide(prepared as described in Example 1) as a starting material, in arelative proportion similar to that used in that Example, the titlecompound was obtained in a 63% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.34-1.50 (2H,multiplet); 1.50-1.64 (4H, multiplet); 1.76-1.98 (1H, broad); 2.28-2.45(4H, multiplet); 3.10 (2H, triplet, J=5.9 Hz); 3.41 (2H, singlet); 3.52(2H, doublet, J=13.9 Hz); 3.79 (1H, doublet, J=13.9 Hz); 4.04-4.16 (4H,multiplet); 4.92 (2H, doublet, J=6.6 Hz); 5.65-5.77 (1H, multiplet);5.82-5.93 (1H, multiplet); 6.75 (1H, singlet); 6.88 (1H, doublet, J=5.3Hz); 7.15-7.34 (1H, broad); 8.06 (1H, doublet, J=5.3 Hz). InfraredAbsorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3300, 2925, 1730, 1670,1610, 1560, 1420, 1400.

The title compound, prepared as described above, was dissolved in ethylacetate and treated with an equimolar amount of a 4N solution ofhydrogen chloride in ethyl acetate to give the hydrochloride of thetitle compound, melting at 111°-114° C.

EXAMPLE 84N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylsulfinyl)acetamide

Following a procedure similar to that described in Example 77, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylthio)acetamide(prepared as described in Example 7) as a starting material, in arelative proportion similar to that used in that Example, the titlecompound was obtained in a 73% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.15 (3H, triplet,J=7.3 Hz); 1.34-1.50 (2H, multiplet); 1.50-1.62 (4H, multiplet);2.28-2.42 (4H, multiplet); 2.37 (2H, quartet, J=7.3 Hz); 3.15 (2H,triplet, J=6.6 Hz); 3.38 (1H, doublet, J=14.2 Hz); 3.41 (2H, singlet);3.73 (1H, doublet, J=14.2 Hz); 4.10 (2H, triplet, J=6.6 Hz); 4.39-4.61(2H, multiplet); 4.93 (2H, doublet, J=6.6 Hz); 5.60-5.72 (1H,multiplet); 5.78-5.91 (1H, multiplet); 6.73 (1H, singlet); 6.88 (1H,doublet, J=5.3 Hz); 7.04-7.23 (1H, broad); 8.06 (1H, doublet, J=5.3 Hz).Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ : 3300, 2925, 1740,1670, 1610, 1560, 1420, 1400.

The title compound, prepared as described above, was dissolved in ethylacetate and treated with an equimolar amount of a 4N solution ofhydrogen chloride in ethyl acetate to give the hydrochloride of thetitle compound, melting at 77°-83° C.

EXAMPLE 85N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(4-pyrimidinylthio)butyramide85(a)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(acetylthio)butyramide

0.50 g of sodium hydride (as a 55% w/w dispersion in mineral oil) wasadded to 80 ml of dimethylformamide under an atmosphere of nitrogen gas,and then 10 ml of a dimethylformamide solution containing 0.81 ml ofthioacetic acid was added to the resulting mixture. The mixture was thenstirred at room temperature for 30 minutes. At the end of this time, 30ml of a dimethylformamide solution containing 3.79 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide(prepared as described in Preparation 2) were added to the mixture, andthe mixture was stirred at room temperature for 2 hours. Ethyl acetatewas then added to the reaction mixture, which was then washed with asaturated aqueous solution of sodium hydrogencarbonate and water. Thesolvent was removed by distillation under reduced pressure, and theresidue was purified by column chromatography through silica gel, usinga 1:19 by volume mixture of methanol and ethyl acetate as the eluent, togive 5.04 g (a quantitative yield) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.50 1.63 (4H, multiplet); 1.93 (2H, quintet, J=7.3 Hz);2.26 (2H, triplet, J=7.3 Hz); 2.29-2.42 (4H, multiplet); 2.91 (2H,triplet, J=7.3 Hz); 3.41 (2H, singlet); 4.03 (2H, triplet, J=5,9 Hz);4.93 (2H, triplet, J=5.9 Hz); 5.61-5.75 (1H, multiplet); 5.78-5.89 (1H,multiplet); 6.09-6.34 (1H, broad); 6.73 (1H, singlet); 6.89 (1H,doublet, J=5.3 Hz); 8.04 (1H, doublet, J=5.3 Hz). Infrared AbsorptionSpectrum (CHCl₃) ν_(max) cm⁻¹ : 3450, 3350, 2925, 2800, 1670, 1610,1560, 1520, 1480, 1420, 1400.

85(b) N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(4-pyrimidinylthio)butyramide

A solution of 1.00 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(acetylthio)butyramide[prepared as described in step (a) above] in 10 ml of methanol was addedto a mixture of 0.48 g of 28% w/v methanolic sodium methoxide and 5 mlof methanol, whilst ice-cooling, and the mixture was stirred at the sametemperature for 20 minutes. At the end of this time, 0.28 g of4-chloropyrimidine was added to the mixture and the mixture was heatedunder reflux for 2 hours. The solvent was then removed by evaporationunder reduced pressure, and water was added to the resulting residue,which was then extracted with ethyl acetate. The solvent was removedfrom the extract by distillation under reduced pressure, and the residuewas purified by column chromatography through silica gel, using a 1:9 byvolume mixture of ethanol and chloroform as the eluent, to give 0.65 g(yield 60%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.36-1.50 (2H,multiplet); 1.50-1.65 (4H, multiplet); 2.06 (2H, quintet, J=7.3 Hz);2.29-2.43 (4H, multiplet); 2.37 (2H, triplet, J=7.3 Hz); 3.24 (2H,triplet, J=7.3 Hz); 3.41 (2H, singlet); 4.05 (2H, triplet, J=5,9 Hz);4.93 (2H, doublet, J=6.6 Hz); 5.61-5.76 (1H, multiplet); 5.78-5.90 (1H,multiplet); 6.22-6.44 (1H, broad); 6.73 (1H, singlet); 6.88 (1H,doublet, J=5.3 Hz); 7.17 (2H, doublet, J=5.3 Hz); 8.03 (1H, doublet,J=5.3 Hz); 8.32 (1H, doublet, J=5.3 Hz); 8.91 (1H, singlet). InfraredAbsorption Spectrum (CHCl₃), ν_(max) cm⁻ : 3450, 3300, 2925, 1660, 1610,1570, 1520, 1440, 1420, 1380.

EXAMPLE 86N-[4-(4-Dimethylaminomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-dimethylaminomethyl-2-pyridyloxy)-cis-2-butenylamine and4-pyrazolecarboxylic acid as starting materials, in relative proportionssimilar to those used in that Example, the title compound was obtainedas an oil in a 65% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 2.27 (6H, singlet);3.40 (2H, singlet); 4.22 (2H, triplet, J=5.9 Hz); 4.99 (2H, doublet,J=6.6 Hz); 5.71-5.94 (2H, multiplet); 6.47 (1H, broad singlet); 6.74(1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 7.97 (2H, singlet); 8.07(1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max)cm⁻¹ : 3450, 3170, 2980, 2940, 1640, 1615, 1565, 1510, 1415, 1400, 1290.

EXAMPLE 87N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-3,5-dimethylpyrrole-2-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine and3,5-dimethylpyrrole-2-carboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as crystals, melting 140°-141° C., in a 58% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.48 (2H,multiplet); 1.50-1.61 (4H, multiplet); 2.23 (3H, singlet); 2.26 (2H,singlet); 2.30-2.42 (4H, multiplet); 3.40 (2H, singlet); 4.22 (2H,triplet, J=5.6 Hz); 4.96 (2H, doublet, J=6.6 Hz); 5.66-5.79 (3H,multiplet); 5.82-5.92 (1H, multiplet); 6.73 (1H, singlet); 6.87 (1H,doublet, J=5.3 Hz); 8.04 (1H, doublet, J=5.3 Hz); 9.13-9.27 (1H, broad).Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3249, 1612, 1525,1410, 1272, 1035, 826.

EXAMPLE 88N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-methylfuran-3-carboxamide

Following a procedure similar to that described in Example 13, but using4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine and2-methylfuran-3-carboxylic acid as starting materials, in relativeproportions similar to those used in that Example, the title compoundwas obtained as an oil in a 77% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.39-1.51 (2H,multiplet); 1.53-1.66 (4H, multiplet); 2.31-2.45 (4H, multiplet); 2.58(3H, singlet); 3.42 (2H, singlet); 4.17 (2H, triplet, J=6.4 Hz); 4.97(2H, doublet, J=6.4 Hz); 5.71-5.81 (1H, multiplet); 5.83-5.93 (1H,multiplet); 6.01-6.18 (1H, broad); 6.41 (1H, doublet, J=2.2 Hz); 6.75(1H, singlet); 6.90 (1H, doublet, J=5.4 Hz); 7.23 (1H, doublet, J=2.2Hz); 8.03 (1H, doublet, J=5.4 Hz). Infrared Absorption Spectrum (liquidfilm), ν_(max) cm⁻¹ : 3325, 2936, 1636, 1611, 1561, 1523, 1420, 1402,1301, 1290, 1039.

The title compound, prepared as described above, was dissolved in ethylacetate and treated with an equimolar amount of a 4N solution ofhydrogen chloride in ethyl acetate to give the hydrochloride of thetitle compound, melting at 258°-261° C. (with decomposition).

EXAMPLE 89N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyrimidinylsulfinyl)butyramide

Following a procedure similar to that described in Example 77, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyrimidinylthio)butyramide(prepared as described in Example 34) as a starting material, in arelative proportion similar to that used in that Example, the titlecompound was obtained as an oil in a 55% yield.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.52-1.63 (4H, multiplet); 1.99-2.12 (1H, multiplet);2.20-2.45 (7H, multiplet); 3.10-3.32 (2H, multiplet); 3.41 (2H,singlet); 4.01 (2H, doublet, J=6.3 Hz); 4.91 (2H, doublet, J=6.6 Hz);5.61-5.71 (1H, multiplet); 5.78-5.87 (1H, multiplet); 6.32 (1H, broadsinglet); 6.73 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 7.41 (1H,triplet, J=4.6 Hz); 8.03 (1H, doublet, J=5.3 Hz); 8.89 (2H, doublet,J=4.6 Hz). Infrared Absorption Spectrum (liquid film), ν_(max) cm⁻¹ :3302, 2936, 1657, 1612, 1561, 1420, 1403, 1384, 1312, 1300, 1289, 1062,1040, 753.

EXAMPLE 90N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylthio)acetamide

Following a procedure similar to that described in Example 2, but usingN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide(prepared as described in Example 1) and propionic anhydride as startingmaterials, in relative proportions similar to those used in thatExample, the title compound was obtained in a 90% yield.

The nuclear magnetic resonance spectrum and the infrared spectrum of thetitle compound are identical with those of the compound prepared asdescribed in Example 7.

PREPARATION 1N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-chloroacetamide

1.00 g of 4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine wasdissolved in 20 ml of ethyl acetate. 0.54 ml of triethylamine was addedto the solution, and the resulting mixture was cooled in an ice bath.0.31 ml of 2-chloroacetyl chloride was added, and the mixture wasstirred for 1 hour at room temperature. At the end of this time, waterwas added, and the reaction mixture was extracted with ethyl acetate.The extract was condensed by evaporation under reduced pressure, and theresidue was purified by silica gel chromatography, eluted with a 1:19 byvolume mixture of methanol and ethyl acetate, to give 0.94 g (yield 73%)of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.50-1.64 (4H, multiplet); 2.30-2.43 (2H, multiplet); 3.41(2H, singlet); 4.06 (2H, singlet); 4.11 (2H, triplet, J=6.6 Hz); 4.94(2H, doublet, J=6.6 Hz); 5.62-5.75 (1H, multiplet); 5.84-5.97 (1H,multiplet); 6.69-6.92 (1H, broad); 6.74 (1H, singlet); 6.88 (1H,doublet, J=4.6 Hz); 8.06 (1H, doublet, J=4.6 Hz). Infrared AbsorptionSpectrum (CHCl₃), ν_(max) cm⁻¹ : 3420, 2920, 1665, 1610, 1525, 1400,1285.

PREPARATION 2N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-chlorobutyramide

Following a procedure similar to that described in Preparation 1, butusing 4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine and4-chlorobutyryl chloride as starting materials, in relative proportionssimilar to those used in that Preparation, the title compound wasobtained at a yield of 73%.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.35-1.53 (2H,multiplet); 1.53-1.78 (4H, multiplet); 2.06-2.17 (2H, multiplet);2.33-2.41 (2H, multiplet); 2.41-2.52 (4H, multiplet); 3.50 (2H,singlet); 3.61 (2H, triplet, J=6.1 Hz); 4.04 (2H, triplet, J=6.1 Hz);4.93 (2H, doublet, J=6.8 Hz); 5.62-5.73 (1H, multiplet); 5.77-5.89 (1H,multiplet); 6.07 (1H, doublet, J=4.9 Hz); 6.08-6.26 (1H, broad); 6.78(1H, singlet); 6.95 (1H, doublet, J=4.9 Hz). Infrared AbsorptionSpectrum (CHCl₃), ν_(max) cm⁻¹ : 3440, 2920, 1660, 1610, 1415, 1295.

PREPARATION 3N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-3-mercaptopropionamide3(a)N-[4-(4-Piperidinomethyl-2-pyridyloxy]-cis-2-butenyl]-3-(acetylthio)propionamide

1.00 g of 3-(acetylthio)propionic acid, 1.39 g of dicyclohexylcarbodiimide, 1.05 g of 1-hydroxybenzotriazole and 1.76 g of4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenylamine were added to 45ml of dimethylformamide, and the solution was stirred for 5 hours atroom temperature. At the end of this time, ethyl acetate was added tothe reaction mixture, insoluble matter was filtered off, and thefiltrate was washed with a saturated aqueous solution of sodiumhydrogencarbonate and then with water. The reaction mixture was thencondensed by evaporation under reduced pressure, and the resultingresidue was subjected to silica gel chromatography, eluted with a 1:19by volume mixture of methanol and ethyl acetate, to give 1.27 g (yield48%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.30-1.50 (2H,multiplet); 1.50-1.70 (4H, multiplet); 2.28-2.44 (4H, multiplet); 2.32(3H, singlet); 2.50 (2H, triplet, J=6.9 Hz); 3.16 (2H, triplet, J=6.9Hz); 3.41 (2H, singlet); 4.04 (2H, triplet, J=6.3 Hz); 4.93 (2H,doublet, J=6.6 Hz); 5.62-5.74 (1H, multiplet); 5.78-5.90 (1H,multiplet); 6.73 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.03 (1H,doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max) cm⁻¹ :3440, 2930, 1675, 1610, 1415, 1400, 1310, 1295, 1285, 1140.

3(b)N-[4-(4-Piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]3-(mercapto)propionamide

1.0 g ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-3-(acetylthio)propionamide[prepared as described in step (a) above] and 0.49 g of a 28% w/vmethanolic solution of sodium methoxide were added to 20 ml of methanol,whilst ice-cooling, and the mixture was stirred at the same temperaturefor 20 minutes. At the end of this time, 0.15 ml of acetic acid wasadded, and the solvent was removed by distillation under reducedpressure. The residue was dissolved in ethyl acetate, washed with waterand condensed by evaporation under reduced pressure, to obtain 0.76 g(yield 85%) of the title compound as an oil.

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.37-1.50 (2H,multiplet); 1.46-1.96 (1H, broad); 1.50-1.65 (4H, multiplet); 2.27-2.43(4H, multiplet); 2.51 (2H, triplet, J=6.9 Hz); 2.83 (2H, doublet oftriplets, J=6.9 & 7.9 Hz); 3.41 (2H, singlet); 4.06 (2H, triplet, J=5.9Hz); 4.94 (2H, doublet, J=6.6 Hz); 5.63-5.77 (1H, multiplet); 5.79-5.90(1H, multiplet); 6.74 (1H, singlet); 6.89 (1H, doublet, J=5.3 Hz); 8.04(1H, doublet, J=5.3 Hz). Infrared Absorption Spectrum (CHCl₃), ν_(max)cm⁻¹ : 3450, 2940, 1665, 1612, 1418, 1400, 1300, 1290.

PREPARATION 4 Ethyl 4-Hydroxy-3-isoxazolecarboxylate

144 g of urea were added to 1 liter of a dimethylformamide solutioncontaining 72 g of ethyl 4-bromo-2-hydroxyimino-3-oxobutyrate. Thereaction solution was heated for 15 minutes at 100° C. and then cooled,after which water was added to the reaction solution, and the mixturewas extracted with ethyl acetate. The extract was washed with diluteaqueous hydrochloric acid and with a saturated aqueous solution ofsodium chloride, in that order, after which it was dried over anhydroussodium sulfate. The solvent was then removed by distillation underreduced pressure, and a 1:1 by volume mixture of ethyl acetate andhexane was added to the residue, to remove insoluble materials. Thesolution thus obtained was purified by silica gel chromatography, elutedwith a 1:4 by volume mixture of ethyl acetate and hexane, to give 19 gof the title compound, melting at 59°-60° C. (after recrystallizationfrom a mixture of ethyl acetate and hexane).

Nuclear Magnetic Resonance Spectrum (CDCl₃), δ ppm: 1.42 (3H, triplet,J=8.0 Hz); 4.48 (2H, quartet, J=8.0 Hz); 6.72 (1H, broad); 8.32 (1H,singlet). Infrared Absorption Spectrum (KBr), ν_(max) cm⁻¹ : 3420, 1718,1140.

We claim:
 1. A compound of formula (I): ##STR6## wherein: R¹ representsacyclic amino group having from 3 to 7 ring atoms, of which from 1 to 3are nitrogen atoms, 0 or 1 is an oxygen atom or a sulfur atom, and theremainder are carbon atoms, or a dialkylamino group in which each alkylgroup is independently selected from the group consisting of alkylgroups having from 1 to 4 carbon atoms; R² representsa group of formula--NHCHR³ R⁴, whereinR³ and R⁴ are independently selected from the groupconsisting of alkyl groups having from 1 to 6 carbon atoms, aryl groupsas defined below and aralkyl groups as defined below,or R³ and R⁴together with the carbon atom to which they are attached, represent acycloalkyl group having from 3 to 8 ring carbon atoms, which group isunsubstituted or is substituted by at least one substituent selectedfrom the group consisting of substituents α, an aromatic heterocyclicgroup having 5 ring atoms, of which from 1 to 3 are hetero-atomsselected from the group consisting of nitrogen, oxygen and sulfurhetero-atoms, said group being unsubstituted or having at least onesubstituent selected, in the case of substituents on carbon atoms, fromthe group consisting of substituents α and, in the case of substituentson nitrogen atoms, from the group consisting of substituents β, or agroup of formula --B--S(O)_(m) --R⁵, whereinR⁵ represents: a substitutedalkyl group which has from 1 to 4 carbon atoms and which is substitutedby at least one substituent selected from the group consisting ofsubstituents γ; or an aromatic heterocyclic group which has 5 or 6 ringatoms of which from 1 to 4 are hetero-atoms selected from the groupconsisting of nitrogen, oxygen and sulfur hetero-atoms, said group beingunsubstituted or having at least one substituent selected, in the caseof substituents on carbon atoms, from the group consisting ofsubstituents α and, in the case of substituents on nitrogen atoms, fromthe group consisting of substituents ε, B represents an alkylene oralkylidene group having from 1 to 6 carbon atoms, and m is 0, 1 or 2; Arepresents a group of formula --CH═CH-- or --(CH₂)_(n) --, where n is 1,2 or 3; said aryl groups are carbocyclic aromatic groups having from 6to 10 ring carbon atoms which are unsubstituted or which are substitutedby at least one substituent selected from the group consisting ofsubstituents ζ; said aralkyl groups are alkyl groups which have from 1to 4 carbon atoms and which are substituted by from 1 to 3 aryl groupsas defined above; said substituents α are selected from the groupconsisting of: alkyl groups having from 1 to 4 carbon atoms; alkoxygroups having from 1 to 4 carbon atoms; hydroxy groups; halogen atoms;amino groups; monoalkylamino groups in which the alkyl part has from 1to 4 carbon atoms; dialkylamino groups in which each alkyl part isindependently selected from the group consisting of alkyl groups havingfrom 1 to 4 carbon atoms; alkanoylamino groups having from 1 to 5 carbonatoms; arylcarbonylamino groups in which the aryl part is as definedabove; and aryl groups as defined above; said substituents β areselected from the group consisting of alkyl groups having from 1 to 4carbon atoms; said substituents γ are selected from the group consistingof: hydroxy groups; alkanoyloxy groups having from 1 to 5 carbon atoms;substituted alkanoyloxy groups which have from 2 to 5 carbon atoms andwhich are substituted by at least one substituent selected from thegroup consisting of substituents δ; arylcarbonyloxy groups in which thearyl part is as defined above; and cycloalkylcarbonyloxy groups in whichthe cycloalkyl part has from 3 to 6 ring carbon atoms and isunsubstituted or is substituted by at least one substituent selectedfrom the group consisting of substituents α; said substituents δ areselected from the group consisting of: carboxy groups; alkoxycarbonylgroups in which the alkoxy part has from 1 to 4 carbon atoms;aryloxycarbonyl groups in which the aryl part is as defined above; andaryl groups as defined above; said substituents ε are selected from thegroup consisting of: alkyl groups having from 1 to 4 carbon atoms; andhydroxyalkyl groups having from 2 to 4 carbon atoms; said substituents ζare selected from the group consisting of substituents α, provided thatany aryl group in said substituents α is not further substituted by anaryl group; PROVIDED THAT, when m is 1, R⁵ represents: said substitutedalkyl group having from 1 to 4 carbon atoms; an aromatic heterocyclicgroup which has 5 ring atoms of which from 2 to 4 are hetero-atomsselected from the group consisting of nitrogen, oxygen and sulfurhetero-atoms, said group being unsubstituted as defined above or anaromatic heterocyclic group which has 6 ring atoms of which from 1 to 4are hetero-atoms selected from the group consisting of nitrogen, oxygenand sulfur hetero-atoms, said group being unsubstituted as definedabove; and pharmaceutically acceptable salts thereof.
 2. The compound ofclaim 1, wherein R¹ represents a cyclic amino group having from 3 to 7ring atoms, of which 1 is a nitrogen atom and the remainder are carbonatoms, or said dialkylamino group.
 3. The compound of claim 2, whereinR¹ represents a cyclic amino group having 5 or 6 ring atoms, of which 1is a nitrogen atom and the remainder are carbon atoms, or saiddialkylamino group.
 4. The compound of claim 3, wherein R¹ represents a1-pyrrolidinyl, piperidino, dimethylamino or diethylamino group.
 5. Thecompound of claim 1, wherein R² represents a group of formula --NHCHR³R⁴, wherein R³ and R⁴ are independently selected from the groupconsisting of:alkyl groups having from 1 to 4 carbon atoms, phenylgroups which are unsubstituted or have at least one substituent selectedfrom the group consisting of substituents ζ, defined in claim 1, andbenzyl and phenethyl groups;or R³ and R⁴ together with the carbon atomto which they are attached, represent a cycloalkyl group having from 3to 6 ring carbon atoms.
 6. The compound of claim 1, wherein R²represents an aromatic heterocyclic group having 5 ring atoms, of which1 is a hetero-atom selected from the group consisting of nitrogen,oxygen and sulfur hetero-atoms, there are 0, 1 or 2 additional nitrogenhetero-atoms, and the remaining ring atoms are carbon atoms, said groupbeing unsubstituted or having at least one substituent selected, in thecase of substituents on carbon atoms, from the group consisting ofsubstituents α and, in the case of substituents on nitrogen atoms, fromthe group consisting of substituents β, as defined in claim
 1. 7. Thecompound of claim 6, wherein said aromatic heterocyclic group isselected from the group consisting of furyl, thienyl, pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl,oxadiazolyl and thiadiazolyl groups, which are unsubstituted or aresubstituted as defined in claim
 6. 8. The compound of claim 1, whereinR² represents a group of formula --B--S(O)_(m) --R⁵, wherein:Brepresents an alkylene or alkylidene group having from 1 to 3 carbonatoms; m is 0, 1 or 2; and R⁵ represents: a substituted alkyl groupwhich has from 2 to 4 carbon atoms and which is substituted at its2-position by at least one substituent selected from the groupconsisting of substituents γ; or an aromatic heterocyclic group whichhas 5 or 6 ring atoms of which 1 is a hetero-atom selected from thegroup consisting of nitrogen, oxygen and sulfur hetero-atoms, there are0, 1, 2 or 3 additional nitrogen hetero-atoms, and the remaining ringatoms are carbon atoms, said group being unsubstituted or having atleast one substituent selected, in the case of substituents on carbonatoms, from the group consisting of substituents α and, in the case ofsubstituents on nitrogen atoms, from the group consisting ofsubstituents ε, as defined in claim
 1. 9. The compound of claim 1,wherein A represents a group of formula --CH═CH-- or --(CH₂)_(n) --,where n is 1 or
 2. 10. The compound of claim 1, wherein:R¹ represents a1-pyrrolidinyl, piperidino, dimethylamino or diethylamino group; R²representsa group of formula --NHCHR³ R⁴, whereinR³ and R⁴ areindependently selected from the group consisting of alkyl groups havingfrom 1 to 4 carbon atoms, benzyl groups, phenethyl groups and phenylgroups which are unsubstituted or which are substituted by at least onesubstituent selected from the group consisting of methyl, methoxy,fluorine atoms and chlorine atoms,or R³ and R⁴ together with the carbonatom to which they are attached, represent a cycloalkyl group havingfrom 3 to 6 ring carbon atoms, a furyl, thienyl, pyrrolyl, oxazolyl,isoxazolyl, thiazolyl, pyrazolyl, imidazolyl or thiadiazolyl group,which is unsubstituted or is substituted by at least one substituentselected, in the case of substituents on carbon atoms, from the groupconsisting of substituents α¹ and, in the case of substituents onnitrogen atoms, from the group consisting of methyl and ethyl groups, ora group of formula --B--S(O)_(m) --R⁵, whereinR⁵ represents: asubstituted ethyl or propyl group which is substituted at its 2-positionby at least one substituent selected from the group consisting ofsubstituents γ¹ ; or an imidazolyl, 1,2,4-triazolyl, 1,3,4-oxadiazolyl,1,3,4-thiadiazolyl, tetrazolyl, pyridyl or pyrimidinyl group which isunsubstituted or has at least one substituent selected, in the case ofsubstituents on carbon atoms, from the group consisting of substituentsα¹ and, in the case of substituents on nitrogen atoms, from the groupconsisting of substituents ε¹, B represents an alkylene or alkylidenegroup having from 1 to 3 carbon atoms, and m is 0, 1 or 2; A representsa group of formula --CH═CH-- or --(CH₂)_(n) --, where n is 1 or 2; saidsubstituents α¹ are selected from the group consisting of: methylgroups, ethyl groups, methoxy groups, ethoxy groups, hydroxy groups,chlorine atoms, amino groups; methylamino groups, ethylamino groups,dimethylamino groups, diethylamino groups, alkanoylamino groups havingfrom 1 to 3 carbon atoms, phenyl groups, and substituted phenyl groupsin which the substituent is selected from the group consisting of methylgroups, methoxy groups, chlorine atoms and fluorine atoms; saidsubstituents γ¹ are selected from the group consisting of: hydroxygroups; alkanoyloxy groups having from 1 to 5 carbon atoms; substitutedalkanoyloxy groups which have 3 or 4 carbon atoms and which aresubstituted by at least one substituent selected from the groupconsisting of carboxy, methoxycarbonyl and ethoxycarbonyl groups;phenylacetoxy groups; benzoyloxy groups; and cycloalkylcarbonyloxygroups in which the cycloalkyl part has from 3 to 6 ring carbon atoms;said substituents ε¹ are selected from the group consisting of: methylgroups, ethyl groups, and hydroxyalkyl groups having from 2 to 4 carbonatoms.
 11. The compound of claim 1, wherein:R¹ represents a1-pyrrolidinyl or piperidino group; R² representsa group of formula--NHCHR³ R⁴, whereinR³ and R⁴ are independently selected from the groupconsisting of methyl, ethyl, phenyl and benzyl groups,or R³ and R⁴together with the carbon atom to which they are attached, represent acycloalkyl group having from 3 to 5 ring carbon atoms, a furyl, thienyl,pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolyl or1,2,3-thiadiazolyl group, which is unsubstituted or is substituted by atleast one substituent selected, in the case of substituents on carbonatoms, from the group consisting of substituents α² and, in the case ofsubstituents on nitrogen atoms, from the group consisting of methyl andethyl groups, or a group of formula --B--S(O)_(m) --R⁵, whereinR⁵represents: a substituted ethyl or propyl group which is substituted atits 2-position by at least one substituent selected from the groupconsisting of substituents γ² ; or a 1,2,4-triazolyl, 1,3,4-oxadiazolylor pyrimidinyl group which is unsubstituted or has at least onesubstituent selected, in the case of substituents on carbon atoms, fromthe group consisting of substituents α³ and, in the case of substituentson nitrogen atoms, from the group consisting of methyl and ethyl groups,B represents an alkylene or alkylidene group having from 1 to 3 carbonatoms, and m is 0 or 1; A represents a group of formula --CH═CH-- or--(CH₂)₂ --; said substituents α² are selected from the group consistingof: methyl groups, ethyl groups, methoxy groups, ethoxy groups, hydroxygroups, chlorine atoms, amino groups, acetamido groups and phenylgroups; said substituents α³ are selected from the group consisting of:methyl groups, ethyl groups, methoxy groups, ethoxy groups, hydroxygroups, chlorine atoms, amino groups, and acetamido groups; saidsubstituents γ² are selected from the group consisting of: hydroxygroups; acetoxy groups; propionyloxy groups; substituted alkanoyloxygroups which have 3 or 4 carbon atoms and which are substituted by atleast one substituent selected from the group consisting of carboxy,methoxycarbonyl and ethoxycarbonyl groups; phenylacetoxy groups;benzoyloxy groups; and cycloalkylcarbonyloxy groups in which thecycloalkyl part has from 3 to 6 ring carbon atoms.
 12. The compound ofclaim 1, wherein:R¹ represents a piperidino group; R² representsa groupof formula --NHCHR³ R⁴, whereinR³ and R⁴ are independently selected fromthe group consisting of methyl, ethyl, phenyl and benzyl groups,or R³and R⁴ together with the carbon atom to which they are attached,represent a cycloalkyl group having 3 or 4 ring carbon atoms, a thienyl,pyrrolyl, thiazolyl, pyrazolyl or 1,2,3-thiadiazolyl group, which isunsubstituted or is substituted by at least one substituent selected, inthe case of substituents on carbon atoms, from the group consisting ofsubstituents α⁴ and, in the case of substituents on nitrogen atoms, frommethyl groups, or a group of formula --B--S(O)_(m) --R⁵, whereinBrepresents a methylene group and R⁵ represents: a substituted ethyl orpropyl group which is substituted at its 2-position by at least onesubstituent selected from the group consisting of substituents γ³ ;or Brepresents a trimethylene group and R⁵ represents: a 1,2,4-triazolyl,1,3,4-oxadiazolyl or pyrimidinyl group which is unsubstituted or has atleast one substituent selected, in the case of substituents on carbonatoms, from the group consisting of methyl, hydroxy and amino groups,and, in the case of substituents on nitrogen atoms, from methyl groups,and m is 0; A represents a group of formula --CH═CH--; said substituentsα⁴ are selected from the group consisting of: methyl groups, methoxygroups, hydroxy groups, chlorine atoms and amino groups; saidsubstituents γ³ are selected from the group consisting of: hydroxygroups; acetoxy groups; propionyloxy groups; substituted propionoyloxygroups which are substituted by at least one substituent selected fromthe group consisting of carboxy, methoxycarbonyl and ethoxycarbonylgroups; benzoyloxy groups; and cycloalkylcarbonyloxy groups in which thecycloalkyl part has 5 or 6 ring carbon atoms.
 13. The compound of claim1, wherein:R¹ represents a piperidino group; R² represents:a pyrazolylgroup, which is unsubstituted or is substituted on a carbon atom by atleast one amino substituent, or a group of formula --B--S(O)_(m) --R⁵,whereinB represents a methylene group and R⁵ represents: a substitutedethyl group which is substituted at its 2-position by at least onesubstituent selected from the group consisting of substituents hydroxy,acetoxy, propionyloxy, benzoyloxy, cyclopentylcarbonyloxy andcyclohexylcarbonyloxy groups;or B represents a trimethylene group and R⁵represents: a 2-pyrimidinyl group; and m is 0; A represents a group offormula --CH═CH--.
 14. The compound of claim 1, selected from the groupconsisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamideand pharmaceutically acceptable salts thereof.
 15. The compound of claim1, selected from the group consisting of3-amino-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamideand pharmaceutically acceptable salts thereof.
 16. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 17. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 18. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 19. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-butyryloxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 20. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isobutyryloxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 21. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isovaleryloxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 22. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-phenylacetoxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 23. The compound of claim1, selected from the group consisting of2-{N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]carbamoylmethylthio}ethylhydrogen succinate and pharmaceutically acceptable salts thereof. 24.The compound of claim 1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-benzoyloxyethylthio)acetamide and pharmaceutically acceptable saltsthereof.
 25. The compound of claim 1, selected from the group consistingofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclopentylcarbonyloxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 26. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclohexylcarbonyloxyethylthio)acetamideand pharmaceutically acceptable salts thereof.
 27. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylsulfinyl)acetamideand pharmaceutically acceptable salts thereof.
 28. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylsulfinyl)acetamideand pharmaceutically acceptable salts thereof.
 29. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(3,3-dimethylbutyryloxy)ethylthio]acetamideand pharmaceutically acceptable salts thereof.
 30. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(2,2-dimethylpropionyloxy)ethylthio]acetamideand pharmaceutically acceptable salts thereof.
 31. The compound of claim1, selected from the group consisting ofN-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyrimidinylthio)butyramideand pharmaceutically acceptable salts thereof.
 32. A pharmaceuticalcomposition for the treatment and prophylaxis of ulcerous conditions,which comprises an anti-ulcer compound in admixture with apharmaceutically acceptable carrier or diluent, wherein the anti-ulcercompound is selected from the group consisting of compounds of formula(I) and pharmaceutically acceptable salts thereof, as claimed inclaim
 1. 33. The composition of claim 32, wherein:R¹ represents apiperidino group; R² representsa group of formula --NHCHR³ R⁴, whereinR³and R⁴ are independently selected from the group consisting of methyl,ethyl, phenyl and benzyl groups,or R³ and R⁴, together with the carbonatom to which they are attached, represent a cycloalkyl group having 3or 4 ring carbon atoms, a thienyl, pyrrolyl, thiazolyl, pyrazolyl or1,2,3-thiadiazolyl group, which is unsubstituted or is substituted by atleast one substituent selected, in the case of substituents on carbonatoms, from the group consisting of substituents α⁴ and, in the case ofsubstituents on nitrogen atoms, from methyl groups, or a group offormula --B--S(O)_(m) --R⁵, whereinB represents a methylene group and R⁵represents: a substituted ethyl or propyl group which is substituted atits 2-position by at least one substituent selected from the groupconsisting of substituents γ³ ;or B represents a trimethylene group andR⁵ represents: a 1,2,4-triazolyl, 1,3,4-oxadiazolyl or pyrimidinyl groupwhich is unsubstituted or has at least one substituent selected, in thecase of substituents on carbon atoms, from the group consisting ofmethyl, hydroxy and amino groups, and, in the case of substituents onnitrogen atoms, from methyl groups, and m is 0; A represents a group offormula --CH═CH--; said substituents α⁴ are selected from the groupconsisting of: methyl groups, methoxy groups, hydroxy groups, chlorineatoms and amino groups; said substituents γ³ are selected from the groupconsisting of: hydroxy groups; acetoxy groups; propionyloxy groups;substituted propionoyloxy groups which are substituted by at least onesubstituent selected from the group consisting of carboxy,methoxycarbonyl and ethoxycarbonyl groups; benzoyloxy groups; andcycloalkylcarbonyloxy groups in which the cycloalkyl part has 5 or 6ring carbon atoms.
 34. The composition of claim 32, wherein:R¹represents a piperidino group; R² represents:a pyrazolyl group, which isunsubstituted or is substituted on a carbon atom by at least one aminosubstituent, or a group of formula --B--S(O)_(m) --R⁵, whereinBrepresents a methylene group and R⁵ represents: a substituted ethylgroup which is substituted at its 2-position by at least one substituentselected from the group consisting of substituents hydroxy, acetoxy,propionyloxy, benzoyloxy, cyclopentylcarbonyloxy andcyclohexylcarbonyloxy groups;or B represents a trimethylene group and Rrepresents: a 2-pyrimidinyl group; and m is 0; A represents a group offormula --CH═CH--.
 35. The composition of claim 32, wherein saidanti-ulcer compound is selected from the group consistingof:N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-pyrazole-4-carboxamide;3-amino-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-butyryloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isobutyryloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isovaleryloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-phenylacetoxyethylthio)acetamide;2-{N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]carbamoylmethylthio}ethylhydrogen succinate;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-benzoyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclopentylcarbonyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclohexylcarbonyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylsulfinyl)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylsulfinyl)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(3,3-dimethylbutyryloxy)ethylthio]acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(2,2-dimethylpropionyloxy)ethylthio]acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyrimidinylthio)butyramide;and pharmaceutically acceptable salts thereof.
 36. A method for thetreatment and prophylaxis of ulcerous conditions, which comprisesadministering an effective amount of an anti-ulcer compound to a mammal,wherein the anti-ulcer compound is selected from the group consisting ofcompounds of formula (I) and pharmaceutically acceptable salts thereof,as claimed in claim
 1. 37. The method of claim 36, wherein:R¹ representsa piperidino group; R² representsa group of formula --NHCHR³ R⁴,whereinR³ and R⁴ are independently selected from the group consisting ofmethyl, ethyl, phenyl and benzyl groups,or R³ and R⁴ together with thecarbon atom to which they are attached, represent a cycloalkyl grouphaving 3 or 4 ring carbon atoms, a thienyl, pyrrolyl, thiazolyl,pyrazolyl or 1,2,3-thiadiazolyl group, which is unsubstituted or issubstituted by at least one substituent selected, in the case ofsubstituents on carbon atoms, from the group consisting of substituentsα⁴ and, in the case of substituents on nitrogen atoms, from methylgroups, or a group of formula --B--S(O)_(m) --R⁵, whereinB represents amethylene group and R⁵ represents: a substituted ethyl or propyl groupwhich is substituted at its 2-position by at least one substituentselected from the group consisting of substituents γ³ ;or B represents atrimethylene group and R⁵ represents: a 1,2,4-triazolyl,1,3,4-oxadiazolyl or pyrimidinyl group which is unsubstituted or has atleast one substituent selected, in the case of substituents on carbonatoms, from the group consisting of methyl, hydroxy and amino groups,and, in the case of substituents on nitrogen atoms, from methyl groups,and m is 0; A represents a group of formula --CH═CH--; said substituentsα⁴ are selected from the group consisting of: methyl groups, methoxygroups, hydroxy groups, chlorine atoms and amino groups; saidsubstituents γ³ are selected from the group consisting of: hydroxygroups; acetoxy groups; propionyloxy groups; substituted propionoyloxygroups which are substituted by at least one substituent selected fromthe group consisting of carboxy, methoxycarbonyl and ethoxycarbonylgroups; benzoyloxy groups; and cycloalkylcarbonyloxy groups in which thecycloalkyl part has 5 or 6 ring carbon atoms.
 38. The method of claim36, wherein:R¹ represents a piperidino group; R² represents:a pyrazolylgroup, which is unsubstituted or is substituted on a carbon atom by atleast one amino substituent, or a group of formula --B--S(O)_(m) --R⁵,whereinB represents a methylene group and R⁵ represents: a substitutedethyl group which is substituted at its 2-position by at least onesubstituent selected from the group consisting of substituents hydroxy,acetoxy, propionyloxy, benzoyloxy, cyclopentylcarbonyloxy andcyclohexylcarbonyloxy groups;or B represents a trimethylene group and R⁵represents: a 2-pyrimidinyl group; and m is 0; A represents a group offormula --CH═CH--.
 39. The method of claim 36, wherein said anti-ulcercompound is selected from the group consistingof:N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-pyrazole-4-carboxamide;3-amino-N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]pyrazole-4-carboxamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-acetoxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-butyryloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isobutyryloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-isovaleryloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-phenylacetoxyethylthio)acetamide;2-{N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-carbamoylmethylthio}ethylhydrogen succinate;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-benzoyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclopentylcarbonyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-cyclohexylcarbonyloxyethylthio)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-hydroxyethylsulfinyl)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-(2-propionyloxyethylsulfinyl)acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(3,3-dimethylbutyryloxy)ethylthio]acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-2-[2-(2,2-dimethylpropionyloxy)ethylthio]acetamide;N-[4-(4-piperidinomethyl-2-pyridyloxy)-cis-2-butenyl]-4-(2-pyrimidinylthio)butyramide;and pharmaceutically acceptable salts thereof.